Stuart Schreiber

Q: What Schools Are Affiliated With Stuart Schreiber

Stuart Schreiber is affiliated with the following schools: University of California, Berkeley, Yale University, University of Salerno, Riken, Princeton University, Stanford University, Massachusetts Institute of Technology, University of Virginia, University of Texas Southwestern Medical Center, Harvard University

Stuart Schreiber's AcademicInfluence.com Rankings

Stuart Schreiber

Chemistry

#190

World Rank

#406

Historical Rank

#101

USA Rank

Organic Chemistry

#25

World Rank

#39

Historical Rank

#14

USA Rank

chemistry Degrees

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Chemistry

Stuart Schreiber's Degrees

PhD Chemistry Princeton University

Why Is Stuart Schreiber Influential?

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According to Wikipedia, Stuart Schreiber, Ph.D. is the Morris Loeb Research Professor at Harvard University, a co-Founder of the Broad Institute, Howard Hughes Medical Institute Investigator, Emeritus, and a member of the National Academy of Sciences and National Academy of Medicine. His work integrates chemical biology and human biology to advance the science of therapeutics. Key advances include the discovery that small molecules can function as “molecular glues” that promote protein–protein interactions, the co-discovery of mTOR and its role in nutrient-response signaling, the discovery of histone deacetylases and the demonstration that chromatin marks regulate gene expression, the development and application of diversity-oriented synthesis to microbial therapeutics, and the discovery of vulnerabilities of cancer cells linked to genetic, lineage and cell-state features, including ferroptotic vulnerabilities. His notable awards include the Wolf Prize in Chemistry and the Arthur Cope Award. His approach to discovering new therapeutics guided many biotechnology companies that he founded, including Vertex Pharmaceuticals and Ariad Pharmaceuticals. He has founded or co-founded 14 biotechnology companies, which have developed 16 first-in-human approved drugs or advanced clinical candidates.

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Stuart Schreiber's Published Works

Number of citations in a given year to any of this author's works

Total number of citations to an author for the works they published in a given year. This highlights publication of the most important work(s) by the author

Published Works

A Bivalent Chromatin Structure Marks Key Developmental Genes in Embryonic Stem Cells (2006) (5120)
Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes (1991) (3800)
Regulation of Ferroptotic Cancer Cell Death by GPX4 (2014) (3053)
The M2 splice isoform of pyruvate kinase is important for cancer metabolism and tumour growth (2008) (2530)
Active genes are tri-methylated at K4 of histone H3 (2002) (2114)
A mammalian protein targeted by G1-arresting rapamycin–receptor complex (1994) (1904)
A Next Generation Connectivity Map: L1000 Platform and the First 1,000,000 Profiles (2017) (1706)
Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin (1995) (1588)
A Mammalian Histone Deacetylase Related to the Yeast Transcriptional Regulator Rpd3p (1996) (1586)
The mechanism of action of cyclosporin A and FK506. (1992) (1569)
Genomic Maps and Comparative Analysis of Histone Modifications in Human and Mouse (2005) (1564)
Nuclear Receptor Repression Mediated by a Complex Containing SMRT, mSin3A, and Histone Deacetylase (1997) (1337)
Atomic structures of the human immunophilin FKBP-12 complexes with FK506 and rapamycin. (1993) (1202)
Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells (2014) (1176)
Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen. (1999) (1136)
A planning strategy for diversity-oriented synthesis. (2004) (1129)
A receptor for the immuno-suppressant FK506 is a cis–trans peptidyl-prolyl isomerase (1989) (1102)
Domain-selective small-molecule inhibitor of histone deacetylase 6 (HDAC6)-mediated tubulin deacetylation (2003) (1030)
Dependency of a therapy-resistant state of cancer cells on a lipid peroxidase pathway (2017) (911)
Selective killing of cancer cells with a small molecule targeting stress response to ROS (2011) (803)
Structure of the FKBP12-Rapamycin Complex Interacting with Binding Domain of Human FRAP (1996) (798)
Two binding orientations for peptides to the Src SH3 domain: development of a general model for SH3-ligand interactions. (1995) (791)
Methylation of histone H3 Lys 4 in coding regions of active genes (2002) (784)
Histone Deacetylase Activity Is Required for Full Transcriptional Repression by mSin3A (1997) (772)
Drug-tolerant persister cancer cells are vulnerable to GPX4 inhibition (2017) (758)
Three proteins define a class of human histone deacetylases related to yeast Hda1p. (1999) (749)
Histone Variant H2A.Z Marks the 5′ Ends of Both Active and Inactive Genes in Euchromatin (2005) (700)
Chromatin deacetylation by an ATP-dependent nucleosome remodelling complex (1998) (696)
Two distinct signal transmission pathways in T lymphocytes are inhibited by complexes formed between an immunophilin and either FK506 or rapamycin. (1990) (634)
The promise and peril of chemical probes. (2015) (623)
Control of p70 S6 kinase by kinase activity of FRAP in vivo (1995) (617)
Regulation of histone deacetylase 4 and 5 and transcriptional activity by 14-3-3-dependent cellular localization. (2000) (615)
Small-molecule inhibition of proteasome and aggresome function induces synergistic antitumor activity in multiple myeloma. (2005) (593)
Small molecules enhance autophagy and reduce toxicity in Huntington's disease models. (2007) (585)
Rapamycin-modulated transcription defines the subset of nutrient-sensitive signaling pathways directly controlled by the Tor proteins. (1999) (578)
Overexpression of a kinase‐inactive ATR protein causes sensitivity to DNA‐damaging agents and defects in cell cycle checkpoints (1998) (569)
Identification of an 11-kDa FKBP12-rapamycin-binding domain within the 289-kDa FKBP12-rapamycin-associated protein and characterization of a critical serine residue. (1995) (547)
Single-Nucleosome Mapping of Histone Modifications in S. cerevisiae (2005) (546)
Inhibition of T cell signaling by immunophilin-ligand complexes correlates with loss of calcineurin phosphatase activity. (1992) (541)
An Interactive Resource to Identify Cancer Genetic and Lineage Dependencies Targeted by Small Molecules (2013) (533)
Deacetylase enzymes: biological functions and the use of small-molecule inhibitors. (2002) (531)
PIK-Related Kinases: DNA Repair, Recombination, and Cell Cycle Checkpoints (1995) (519)
Identification of a Class of Small Molecule Inhibitors of the Sirtuin Family of NAD-dependent Deacetylases by Phenotypic Screening* (2001) (516)
CoREST is an integral component of the CoREST- human histone deacetylase complex. (2001) (512)
Correlating chemical sensitivity and basal gene expression reveals mechanism of action (2015) (500)
Protein phosphatase 2A interacts with the 70-kDa S6 kinase and is activated by inhibition of FKBP12-rapamycinassociated protein. (1999) (493)
Small molecule developmental screens reveal the logic and timing of vertebrate development. (2000) (484)
A small molecule that directs differentiation of human ESCs into the pancreatic lineage. (2009) (479)
Harnessing Connectivity in a Large-Scale Small-Molecule Sensitivity Dataset. (2015) (472)
Towards the optimal screening collection: a synthesis strategy. (2008) (455)
Controlling signal transduction with synthetic ligands. (1993) (451)
Genomewide studies of histone deacetylase function in yeast. (2000) (426)
Small molecules efficiently direct endodermal differentiation of mouse and human embryonic stem cells. (2009) (420)
Lactacystin, Proteasome Function, and Cell Fate* (1998) (408)
Signaling Network Model of Chromatin (2002) (397)
A Signaling Pathway to Translational Control (1996) (393)
Global nucleosome occupancy in yeast (2004) (393)
Chemical suppression of a genetic mutation in a zebrafish model of aortic coarctation (2004) (381)
Perturbational profiling of a cell-line model of tumorigenesis by using metabolic measurements (2005) (374)
A role for histone deacetylase activity in HDAC1-mediated transcriptional repression. (1998) (372)
A GPX4-dependent cancer cell state underlies the clear-cell morphology and confers sensitivity to ferroptosis (2019) (356)
Nuclear histone acetylases and deacetylases and transcriptional regulation: HATs off to HDACs. (1997) (353)
Chemical genetics resulting from a passion for synthetic organic chemistry. (1998) (353)
Printing Small Molecules as Microarrays and Detecting Protein−Ligand Interactions en Masse (1999) (344)
FKBP12-Rapamycin-associated Protein (FRAP) Autophosphorylates at Serine 2481 under Translationally Repressive Conditions* (2000) (344)
Reduced histone biosynthesis and chromatin changes arising from a damage signal at telomeres (2010) (343)
Dissecting glucose signalling with diversity-oriented synthesis and small-molecule microarrays (2002) (320)
Solution structure of the SH3 domain of Src and identification of its ligand-binding site. (1992) (315)
Direct control of mitochondrial function by mTOR (2009) (314)
TOR kinase domains are required for two distinct functions, only one of which is inhibited by rapamycin (1995) (311)
Immunophilin-sensitive protein phosphatase action in cell signaling pathways (1992) (307)
ATR inhibition selectively sensitizes G1 checkpoint-deficient cells to lethal premature chromatin condensation (2001) (307)
Acceleration of the Dess-Martin Oxidation by Water (1994) (304)
Dimerization as a regulatory mechanism in signal transduction. (1998) (301)
Identifying the proteins to which small-molecule probes and drugs bind in cells (2009) (300)
Atg16L1 T300A variant decreases selective autophagy resulting in altered cytokine signaling and decreased antibacterial defense (2014) (298)
Inhibition of Dihydroorotate Dehydrogenase Overcomes Differentiation Blockade in Acute Myeloid Leukemia (2016) (297)
cDNA cloning and gene mapping of a candidate human cell cycle checkpoint protein. (1996) (287)
Methylation of histone H3 K4 mediates association of the Isw1p ATPase with chromatin. (2003) (286)
Generating Diverse Skeletons of Small Molecules Combinatorially (2003) (283)
A small molecule that binds Hedgehog and blocks its signaling in human cells (2009) (278)
ChemBank: a small-molecule screening and cheminformatics resource database (2007) (275)
Regulatory intramolecular association in a tyrosine kinase of the Tec family (1997) (275)
The landscape of cancer cell line metabolism (2019) (273)
Association of a 59-kilodalton immunophilin with the glucocorticoid receptor complex. (1992) (272)
Identification of the immunophilins capable of mediating inhibition of signal transduction by cyclosporin A and FK506: roles of calcineurin binding and cellular location (1993) (268)
Molecular cloning and overexpression of the human FK506-binding protein FKBP (1990) (265)
Partitioning the transcriptional program induced by rapamycin among the effectors of the Tor proteins (2000) (259)
Plasticity of ether lipids promotes ferroptosis susceptibility and evasion (2020) (258)
Cytochrome P450 oxidoreductase contributes to phospholipid peroxidation in ferroptosis (2020) (256)
Small molecules of different origins have distinct distributions of structural complexity that correlate with protein-binding profiles (2010) (254)
FKBP12-rapamycin-associated protein associates with mitochondria and senses osmotic stress via mitochondrial dysfunction (2002) (251)
Histone Deacetylase 1 Phosphorylation Promotes Enzymatic Activity and Complex Formation* (2001) (250)
Small molecules: the missing link in the central dogma (2005) (249)
Copper-Mediated Amidation of Heterocyclic and Aromatic C−H Bonds (2009) (249)
Organic chemistry: Molecular diversity by design (2009) (247)
Controlling protein association and subcellular localization with a synthetic ligand that induces heterodimerization of proteins. (1996) (245)
Immunosuppressants implicate protein phosphatase regulation of K+ channels in guard cells. (1993) (245)
Significance of HDAC6 regulation via estrogen signaling for cell motility and prognosis in estrogen receptor-positive breast cancer (2005) (241)
Finding new components of the target of rapamycin (TOR) signaling network through chemical genetics and proteome chips. (2004) (237)
A library of spirooxindoles based on a stereoselective three-component coupling reaction. (2004) (234)
Perturbational profiling of nanomaterial biologic activity (2008) (234)
N-oxide promoted pauson-khand cyclizations at room temperature (1990) (231)
Specific interactions outside the proline-rich core of two classes of Src homology 3 ligands. (1995) (230)
Dimeric ligands define a role for transcriptional activation domains in reinitiation (1996) (228)
Dissecting cellular processes using small molecules: identification of colchicine-like, taxol-like and other small molecules that perturb mitosis. (2000) (220)
From Knowing to Controlling: A Path from Genomics to Drugs Using Small Molecule Probes (2003) (218)
Selective killing of cancer cells by a small molecule targeting the stress response to ROS (2012) (217)
Atg16l1 is required for autophagy in intestinal epithelial cells and protection of mice from Salmonella infection. (2013) (210)
Catalytic asymmetric [3+2] cycloaddition of azomethine ylides. Development of a versatile stepwise, three-component reaction for diversity-oriented synthesis. (2003) (207)
A beta-lactone related to lactacystin induces neurite outgrowth in a neuroblastoma cell line and inhibits cell cycle progression in an osteosarcoma cell line. (1994) (207)
The small-molecule approach to biology (2003) (206)
TWO-DIRECTIONAL CHAIN SYNTHESIS AND TERMINUS DIFFERENTIATION (1994) (203)
Pairwise use of complexity-generating reactions in diversity-oriented organic synthesis. (2000) (201)
Depudecin induces morphological reversion of transformed fibroblasts via the inhibition of histone deacetylase. (1998) (199)
Cloning, expression, and purification of human cyclophilin in Escherichia coli and assessment of the catalytic role of cysteines by site-directed mutagenesis. (1990) (198)
Convenient methods for patterning the adhesion of mammalian cells to surfaces using self-assembled monolayers of alkanethiolates on gold (1993) (196)
Integration of growth factor and nutrient signaling: implications for cancer biology. (2003) (194)
Multidimensional chemical genetic analysis of diversity-oriented synthesis-derived deacetylase inhibitors using cell-based assays. (2003) (193)
High-throughput screening of small molecules in miniaturized mammalian cell-based assays involving post-translational modifications. (1999) (191)
Diversity-oriented synthesis yields novel multistage antimalarial inhibitors (2016) (190)
Large-scale chemical dissection of mitochondrial function (2008) (190)
Binding affinity and kinetic analysis of targeted small molecule-modified nanoparticles. (2010) (189)
Alpha 4 associates with protein phosphatases 2A, 4, and 6. (1998) (189)
Total synthesis of FK506 and an FKBP probe reagent, [C(8),C(9)-13C2]-FK506 (1990) (186)
Synthesis, cellular evaluation, and mechanism of action of piperlongumine analogs (2012) (184)
Inducible gene expression and protein translocation using nontoxic ligands identified by a mammalian three-hybrid screen. (1997) (183)
Chemical genetic strategy identifies histone deacetylase 1 (HDAC1) and HDAC2 as therapeutic targets in sickle cell disease (2010) (181)
SIR1, an Upstream Component in Auxin Signaling Identified by Chemical Genetics (2003) (178)
High-throughput identification of genotype-specific cancer vulnerabilities in mixtures of barcoded tumor cell lines (2016) (172)
Vinylogous polypeptides: an alternative peptide backbone (1992) (170)
Understanding and controlling the cell cycle with natural products. (1996) (169)
Inhibition of FKBP rotamase activity by immunosuppressant FK506: twisted amide surrogate. (1990) (166)
Stereoselective Synthesis of over Two Million Compounds Having Structural Features Both Reminiscent of Natural Products and Compatible with Miniaturized Cell-Based Assays (1998) (162)
Multiplex Cytological Profiling Assay to Measure Diverse Cellular States (2013) (160)
Translation control: Connecting mitogens and the ribosome (1998) (159)
Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. (2013) (156)
Reactions that proceed with a combination of enantiotopic group and diastereotopic face selectivity can deliver products with very high enantiomeric excess: experimental support of a mathematical model (1987) (155)
PERSPECTIVE: THE SMALL-MOLECULE APPROACH TO BIOLOGYChemical genetics and diversity-oriented organic synthesis make possible the systematic exploration of biology (2003) (155)
A synthesis strategy yielding skeletally diverse small molecules combinatorially. (2004) (154)
Small Molecule Enhancers of Rapamycin-Induced TOR Inhibition Promote Autophagy, Reduce Toxicity in Huntington’s Disease Models and Enhance Killing of Mycobacteria by Macrophages (2007) (153)
Discovery of an inhibitor of a transcription factor using small molecule microarrays and diversity-oriented synthesis. (2003) (152)
Toward performance-diverse small-molecule libraries for cell-based phenotypic screening using multiplexed high-dimensional profiling (2014) (151)
Synthesis and cellular profiling of diverse organosilicon small molecules. (2007) (150)
FKBP-rapamycin inhibits a cyclin-dependent kinase activity and a cyclin D1-Cdk association in early G1 of an osteosarcoma cell line. (1993) (150)
Total synthesis and biological mode of action of largazole: a potent class I histone deacetylase inhibitor. (2008) (147)
Functional analysis of Fas signaling in vivo using synthetic inducers of dimerization (1996) (147)
Small-Molecule Microarrays: Covalent Attachment and Screening of Alcohol-Containing Small Molecules on Glass Slides (2000) (147)
Phthalascidin, a synthetic antitumor agent with potency and mode of action comparable to ecteinascidin 743. (1999) (146)
Ozonolytic cleavage of cycloalkenes to terminally differentiated products (1983) (141)
Development of small-molecule probes that selectively kill cells induced to express mutant RAS. (2012) (139)
Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles (2020) (138)
Structure and basicity of silyl ethers: a crystallographic and ab initio inquiry into the nature of silicon-oxygen interactions (1990) (137)
A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases. (2011) (137)
Synthesis of Natural and Modified Trapoxins, Useful Reagents for Exploring Histone Deacetylase Function (1996) (137)
Chemical probes and drug leads from advances in synthetic planning and methodology (2018) (133)
Kinase phosphorylation: Keeping it all in the family (1999) (133)
Identification of Regulators of Polyploidization Presents Therapeutic Targets for Treatment of AMKL (2012) (133)
A precision oncology approach to the pharmacological targeting of mechanistic dependencies in neuroendocrine tumors (2018) (133)
Atomic Structure of the Rapamycin Human Immunophilin FKBP-12 Complex (1991) (132)
Three-part inventions: intracellular signaling and induced proximity. (1996) (132)
A Small-Molecule Probe of the Histone Methyltransferase G9a Induces Cellular Senescence in Pancreatic Adenocarcinoma (2012) (132)
Selection of gp41-mediated HIV-1 cell entry inhibitors from biased combinatorial libraries of non-natural binding elements (1999) (131)
(+)-Discodermolide binds to microtubules in stoichiometric ratio to tubulin dimers, blocks taxol binding and results in mitotic arrest. (1996) (131)
Metabolomic adaptations and correlates of survival to immune checkpoint blockade (2019) (130)
Signal transduction in T lymphocytes using a conditional allele of Sos. (1995) (130)
Molecular cloning of a membrane-associated human FK506- and rapamycin-binding protein, FKBP-13. (1991) (130)
Structure-function analysis of SH3 domains: SH3 binding specificity altered by single amino acid substitutions (1995) (129)
Short synthesis of skeletally and stereochemically diverse small molecules by coupling petasis condensation reactions to cyclization reactions. (2006) (128)
Lewis Acid Mediated Version of the Nicholas Reaction: Synthesis of Syn-Alkylated Products and Cobalt-Complexed Cycloalkynes. (1986) (127)
Complete amino acid sequence of the FK506 and rapamycin binding protein, FKBP, isolated from calf thymus (1991) (127)
Enantioselective addition of terminal alkynes to isolated isoquinoline iminiums. (2006) (127)
Fragmentation reactions of .alpha.-alkoxy hydroperoxides and application to the synthesis of the macrolide (.+-.)-recifeiolide (1980) (127)
High-Throughput Assay and Discovery of Small Molecules that Interrupt Malaria Transmission (2016) (125)
Natural Products as Probes of Cellular Function: Studies of Immunophilins (1992) (125)
Synthesis of 7200 small molecules based on a substructural analysis of the histone deacetylase inhibitors trichostatin and trapoxin. (2001) (125)
Structure of the Pl3K SH3 domain and analysis of the SH3 family (1993) (124)
A genetic basis for the variation in the vulnerability of cancer to DNA damage (2016) (124)
Synthesis and Preliminary Evaluation of a Library of Polycyclic Small Molecules for Use in Chemical Genetic Assays (1999) (124)
Rapamycin and FK506 binding proteins (immunophilins) (1991) (123)
Genetic basis of individual differences in the response to small-molecule drugs in yeast (2007) (123)
Stereochemical control of the Passerini reaction. (2004) (123)
Diversity-oriented synthesis of biaryl-containing medium rings using a one bead/one stock solution platform. (2002) (123)
Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes (2017) (122)
Transannular Diels-Alder route to systems related to dynemicin A (1990) (119)
Development and validation of a T7 based linear amplification for genomic DNA (2003) (119)
Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes (2015) (118)
A yeast genetic system for selecting small molecule inhibitors of protein-protein interactions in nanodroplets. (1997) (118)
The Rise of Molecular Glues (2021) (117)
Relationship of stereochemical and skeletal diversity of small molecules to cellular measurement space. (2004) (117)
On the Conformation and Structure of Organometal Complexes in the Solid State: Two Studies Relevant to Chemical Synthesis (1990) (116)
A robust small-molecule microarray platform for screening cell lysates. (2006) (115)
Organic synthesis toward small-molecule probes and drugs (2011) (115)
Dynamic behavior of dicobalt hexacarbonyl propargyl cations and their reactions with chiral nucleophiles (1987) (112)
SYNTHESES OF DISCODERMOLIDES USEFUL FOR INVESTIGATING MICROTUBULE BINDING AND STABILIZATION (1996) (111)
Control of p70 S6 kinase by kinase activity of FRAP in vivo (1995) (111)
Biased combinatorial libraries: novel ligands for the SH3 domain of phosphatidylinositol 3-kinase (1993) (111)
Type 2 Diabetes Variants Disrupt Function of SLC16A11 through Two Distinct Mechanisms (2017) (110)
Immunophilin ligands demonstrate common features of signal transduction leading to exocytosis or transcription. (1991) (110)
GTP-dependent binding of the antiproliferative agent didemnin to elongation factor 1 alpha. (1994) (110)
Integrative radiogenomic profiling of squamous cell lung cancer. (2013) (106)
Total synthesis of the immunosuppressive agent (-)-discodermolide (1993) (106)
Structural biasing elements for in-cell histone deacetylase paralog selectivity. (2003) (105)
Substrate specificity for the human rotamase FKBP: a view of FK506 and rapamycin as leucine-(twisted amide)-proline mimics (1990) (105)
Microarray-based method for monitoring yeast overexpression strains reveals small-molecule targets in TOR pathway (2006) (104)
An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells (2020) (103)
A rapamycin-selective 25-kDa immunophilin. (1992) (103)
Molecular association between ATR and two components of the nucleosome remodeling and deacetylating complex, HDAC2 and CHD4. (1999) (103)
Niche-based screening identifies small-molecule inhibitors of leukemia stem cells. (2013) (102)
Total synthesis of (-)-hikizimycin employing the strategy of two-directional chain synthesis (1992) (101)
ATR Is Not Required for p53 Activation but Synergizes with p53 in the Replication Checkpoint* (2002) (100)
Tandem Use of Cobalt-Mediated Reactions to Synthesize (+)-Epoxydictymene, a Diterpene Containing a Trans-Fused 5−5 Ring System (1997) (100)
Skeletal diversity via a branched pathway: efficient synthesis of 29 400 discrete, polycyclic compounds and their arraying into stock solutions. (2002) (100)
Transmembrane channels based on tartaric acid-gramicidin A hybrids. (1989) (99)
Small-molecule targeting of brachyury transcription factor addiction in chordoma (2019) (98)
Complex α-Pyrones Synthesized by a Gold-Catalyzed Coupling Reaction† (2007) (98)
Fas signal transduction triggers either proliferation or apoptosis in human fibroblasts. (1997) (98)
Synthesis and conformation-activity relationships of the peptide isosteres of FK228 and largazole. (2009) (95)
Reassignment of stereochemistry and total synthesis of the thrombin inhibitor cyclotheonamide B (1992) (94)
Synthesis and histone deacetylase inhibitory activity of largazole analogs: alteration of the zinc-binding domain and macrocyclic scaffold. (2009) (94)
A small-molecule allosteric inhibitor of Mycobacterium tuberculosis tryptophan synthase. (2017) (94)
A cell-based, high-throughput screen for small molecule regulators of hepatitis C virus replication. (2007) (93)
Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma (2016) (93)
Gossypol and an HMT G9a inhibitor act in synergy to induce cell death in pancreatic cancer cells (2013) (92)
Evidence for Protein Phosphatase 1 and 2A Regulation of K+ Channels in Two Types of Leaf Cells (1994) (91)
SnapShot: Ca2+-Calcineurin-NFATSignaling (2009) (90)
Cyclosporine- and FK506-induced sympathetic activation correlates with calcineurin-mediated inhibition of T-cell signaling. (1993) (90)
Fiber-derived butyrate and the prevention of colon cancer. (1997) (89)
The identification of myriocin-binding proteins. (1999) (89)
Carbon- and nitrogen-quality signaling to translation are mediated by distinct GATA-type transcription factors (2001) (89)
Der optimale Molekülsatz für Screening‐Anwendungen: eine Synthesestrategie (2008) (89)
Chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histone and tubulin acetylation. (2003) (88)
The Power of Sophisticated Phenotypic Screening and Modern Mechanism-of-Action Methods. (2016) (86)
A dataset of images and morphological profiles of 30 000 small-molecule treatments using the Cell Painting assay (2017) (86)
An expanded universe of cancer targets (2021) (86)
Evaluating drug targets through human loss-of-function genetic variation (2019) (86)
Crebinostat: A novel cognitive enhancer that inhibits histone deacetylase activity and modulates chromatin-mediated neuroplasticity (2012) (84)
Skeletal diversity via a folding pathway: synthesis of indole alkaloid-like skeletons. (2005) (83)
Total Synthesis of (-)-Rapamycin Using an Evans-Tishchenko Fragment Coupling (1993) (82)
Fluorous-based small-molecule microarrays for the discovery of histone deacetylase inhibitors. (2007) (82)
Rpd3p relocation mediates a transcriptional response to rapamycin in yeast. (2004) (81)
Cyclic AMP Stimulates K+ Channel Activity in Mesophyll Cells of Vicia faba L (1994) (81)
Grb2 SH3 binding to peptides from Sos: evaluation of a general model for SH3-ligand interactions. (1995) (81)
Chemical biology : from small molecules to systems biology and drug design (2007) (81)
Quantifying structure and performance diversity for sets of small molecules comprising small-molecule screening collections (2011) (81)
Cobalt-Mediated Total Synthesis of (+)-Epoxydictymene (1994) (81)
Unifying principles of bifunctional, proximity-inducing small molecules (2020) (81)
Discovery of histone deacetylase 8 selective inhibitors. (2011) (80)
A composite FKBP12-FK506 surface that contacts calcineurin (1993) (80)
Overproduction and dissection of proteins by the expression-cassette polymerase chain reaction. (1990) (80)
Syntheses of α-Pyrones Using Gold-Catalyzed Coupling Reactions (2011) (79)
Carbon metabolism-mediated myogenic differentiation (2009) (79)
Identification and Characterization of Small Molecule Inhibitors of a Class I Histone Deacetylase from Plasmodium falciparum (2009) (79)
Light-regulated, tissue-specific immunophilins in a higher plant. (1994) (79)
A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells (2012) (78)
pCyP B: a chloroplast-localized, heat shock-responsive cyclophilin from fava bean. (1994) (78)
Inhibition of histone deacetylase 3 protects beta cells from cytokine-induced apoptosis. (2012) (78)
A Strategy for Macrocyclic Ring Closure and Functionalization Aimed toward Split-Pool Syntheses (1999) (77)
The effect of the immunosuppressant FK‐506 on alternate pathways of T cell activation (1991) (77)
STK33 kinase inhibitor BRD-8899 has no effect on KRAS-dependent cancer cell viability (2012) (77)
Molecular characterization of a FKBP-type immunophilin from higher plants. (1996) (77)
The epoxidation of unsaturated macrolides. Stereocontrolled routes to ionophore subunits (1986) (77)
Synthesis of a Bicyclic Azetidine with In Vivo Antimalarial Activity Enabled by Stereospecific, Directed C(sp3)–H Arylation (2017) (77)
Controlling programmed cell death with a cyclophilin-cyclosporin-based chemical inducer of dimerization. (1996) (76)
Identification of a selective small molecule inhibitor of breast cancer stem cells. (2012) (76)
Gold(I)-Catalyzed Coupling Reactions for the Synthesis of Diverse Small Molecules Using the Build/Couple/Pair Strategy (2009) (76)
A Compendium of Genetic Modifiers of Mitochondrial Dysfunction Reveals Intra-organelle Buffering (2019) (76)
Expanding the functional group compatibility of small-molecule microarrays: discovery of novel calmodulin ligands. (2003) (75)
The kinase DYRK1A reciprocally regulates the differentiation of Th17 and regulatory T cells (2015) (75)
Criegee rearrangement of α-alkoxy hydroperoxides a synthesis of esters and lactones that complements the baeyer-villiger oxidation of ketones (1983) (75)
High-Throughput Luciferase-Based Assay for the Discovery of Therapeutics That Prevent Malaria (2016) (73)
Rational Design of Orthogonal Receptor - Ligand Combinations** (1995) (73)
The PIK-related kinases intercept conventional signaling pathways. (1999) (73)
Convergent diversity-oriented synthesis of small-molecule hybrids. (2005) (72)
FKBP54, a novel FK506-binding protein in avian progesterone receptor complexes and HeLa extracts. (1993) (72)
Total synthesis of (±)-asteltoxin (1984) (71)
Proximity and orientation underlie signaling by the non‐receptor tyrosine kinase ZAP70 (1997) (71)
Small-molecule inducers of insulin expression in pancreatic α-cells (2010) (70)
A general strategy for producing conditional alleles of Src-like tyrosine kinases. (1995) (70)
Stereochemical control of skeletal diversity. (2003) (70)
Distinct Biological Network Properties between the Targets of Natural Products and Disease Genes (2010) (69)
[2 + 2] photocycloadditions in the synthesis of chiral molecules. (1985) (69)
Protein Structure-Based Combinatorial Chemistry: Discovery of Non-Peptide Binding Elements to Src SH3 Domain (1996) (69)
Antisense oligonucleotides extend survival of prion-infected mice (2019) (69)
Cyclobutene bridgehead olefin route to the American cockroach sex pheromone, periplamone, periplanone-B (1984) (69)
Syntheses of aminoalcohol-derived macrocycles leading to a small-molecule binder to and inhibitor of Sonic Hedgehog. (2009) (68)
Vector algebra in the analysis of genome-wide expression data (2002) (68)
Target of rapamycin proteins and their kinase activities are required for meiosis. (1997) (66)
Synthetic studies in the brefeldin series: asymmetric enamine-enal cycloaddition and intramolecular Nozaki reactions (1988) (65)
Proximity versus allostery: the role of regulated protein dimerization in biology. (1994) (65)
Identification of cancer cytotoxic modulators of PDE3A by predictive chemogenomics (2015) (65)
Towards patient-based cancer therapeutics (2010) (65)
Crystal structures of cyclophilin A complexed with cyclosporin A and N-methyl-4-[(E)-2-butenyl]-4,4-dimethylthreonine cyclosporin A. (1994) (65)
Effects of cyclosporin A and FK506 on Fc epsilon receptor type I-initiated increases in cytokine mRNA in mouse bone marrow-derived progenitor mast cells: resistance to FK506 is associated with a deficiency in FK506-binding protein FKBP12. (1992) (63)
Structure-based design of a cyclophilin-calcineurin bridging ligand. (1993) (63)
Synthesis of the bicyclic core of the esperamicin/calichemicin class of antitumor agents (1988) (63)
A miniaturized arrayed assay format for detecting small molecule-protein interactions in cells. (1997) (62)
An oligomer-based approach to skeletal diversity in small-molecule synthesis. (2006) (62)
Towards Diversity-Oriented, Stereoselective Syntheses of Biaryl- or Bis(aryl)metal-Containing Medium Rings (2000) (61)
Site-specific atom transfer from DNA to a bound ligand defines the geometry of a DNA-calicheamicin .gamma.1I complex (1990) (61)
Small molecules, big players: the National Cancer Institute's Initiative for Chemical Genetics. (2006) (61)
NAMPT Is the Cellular Target of STF-31-Like Small-Molecule Probes (2014) (60)
Small-molecule screening identifies inhibition of salt-inducible kinases as a therapeutic strategy to enhance immunoregulatory functions of dendritic cells (2014) (60)
Structure of guanine-nucleotide-exchange factor human Mss4 and identification of its Rab-interacting surface (1995) (59)
Single-Step Synthesis of Cell-Permeable Protein Dimerizers That Activate Signal Transduction and Gene Expression (1997) (59)
Two-directional chain synthesis : an application to the synthesis of (+)-mycoticin A (1993) (59)
The cell cycle, signal transduction, and immunophilin-ligand complexes (1993) (59)
Immunophilin-ligand complexes as probes of intracellular signaling pathways. (1991) (58)
Discovery of Small-Molecule Enhancers of Reactive Oxygen Species That are Nontoxic or Cause Genotype-Selective Cell Death (2013) (58)
Synthetic strategy toward skeletal diversity via solid-supported, otherwise unstable reactive intermediates. (2004) (58)
Selective modulation of autophagy, innate immunity, and adaptive immunity by small molecules. (2013) (58)
Chemical genomic profiling of biological networks using graph theory and combinations of small molecule perturbations. (2003) (57)
Application of the two-directional chain synthesis strategy to the first stereochemical assignment of structure to members of the skipped-polyol polyene macrolide class: mycoticin A and B (1987) (57)
Asymmetric Catalysis in Diversity-Oriented Organic Synthesis: Enantioselective Synthesis of 4320 Encoded and Spatially Segregated Dihydropyrancarboxamides We thank the National Institute of General Medical Sciences (GM-52067) for support of this research, and Dr. John Tallarico and Max Narovlyansky (2001) (56)
Synthesis and analysis of 506BD, a high-affinity ligand for the immunophilin FKBP (1991) (56)
Small-molecule enhancers of autophagy modulate cellular disease phenotypes suggested by human genetics (2015) (56)
Sequential assignment and structure determination of spider toxin omega-Aga-IVB. (1993) (56)
Linking tumor mutations to drug responses via a quantitative chemical-genetic interaction map. (2015) (55)
Structural and synthetic studies of the spore germination autoinhibitor, gloeosporone. (1988) (55)
ENANTIOSPECIFIC TOTAL SYNTHESIS OF THE PROTEIN PHOSPHATASE INHIBITOR MOTUPORIN (1995) (55)
Total syntheses of Di- and tri-O-methyl dynemicin A methyl esters (1993) (55)
Empirical Bayes Analysis of Quantitative Proteomics Experiments (2009) (55)
Application of the furan carbonyl photocycloaddition reaction to the synthesis of the bis(tetrahydrofuran) moiety of asteltoxin (1983) (54)
P59 (FK506 binding protein 59) interaction with heat shock proteins is highly conserved and may involve proteins other than steroid receptors. (1993) (54)
1H and 15N assignments and secondary structure of the Src SH3 domain (1993) (54)
Targeting Dependency on the GPX4 Lipid Peroxide Repair Pathway for Cancer Therapy. (2018) (54)
Diacylfuroxans Are Masked Nitrile Oxides That Inhibit GPX4 Covalently. (2019) (53)
A Human Islet Cell Culture System for High-Throughput Screening (2012) (53)
Synthetic studies of the furan-carbonyl photocycloaddition reaction: a total synthesis of (±)-avenaciolide (1984) (53)
Split--pool synthesis of 1,3-dioxanes leading to arrayed stock solutions of single compounds sufficient for multiple phenotypic and protein-binding assays. (2001) (53)
A chemical biology view of bioactive small molecules and a binder-based approach to connect biology to precision medicines (2018) (52)
Molecular basis for the binding of SH3 ligands with non-peptide elements identified by combinatorial synthesis. (1996) (52)
Aldehyde dehydrogenase 3a2 protects AML cells from oxidative death and the synthetic lethality of ferroptosis inducers. (2020) (52)
DNA barcoding a complete matrix of stereoisomeric small molecules. (2018) (51)
Potentiation of progesterone receptor-mediated transcription by the immunosuppressant FK506. (1994) (51)
Replication and Active Demethylation Represent Partially Overlapping Mechanisms for Erasure of H3K4me3 in Budding Yeast (2010) (51)
Small molecule-dependent genetic selection in stochastic nanodroplets as a means of detecting protein-ligand interactions on a large scale. (1997) (50)
The DNA damage mark pH2AX differentiates the cytotoxic effects of small molecule HDAC inhibitors in ovarian cancer cells (2011) (50)
Catalytic diastereoselective petasis reactions. (2011) (50)
Small-molecule fluorophores to detect cell-state switching in the context of high-throughput screening. (2008) (50)
Design, synthesis, and properties of a photoactivatable membrane-spanning phospholipidic probe (1993) (50)
Prion protein lowering is a disease-modifying therapy across prion disease stages, strains and endpoints (2020) (49)
Didemnin binds to the protein palmitoyl thioesterase responsible for infantile neuronal ceroid lipofuscinosis. (1996) (49)
Application of the allylic diazene rearrangement: synthesis of the enediyne-bridged tricyclic core of dynemicin A (1992) (49)
A boronic ester annulation strategy for diversity-oriented organic synthesis. (2002) (49)
Model of the interactions of calichemicin gamma 1 with a DNA fragment from pBR322. (1989) (49)
Phosphorylation-Inducing Chimeric Small Molecules. (2020) (48)
Mechanistic studies of a signaling pathway activated by the organic dimerizer FK1012. (1994) (48)
Small-molecule diversity using a skeletal transformation strategy. (2005) (48)
DiSCoVERing Innovative Therapies for Rare Tumors: Combining Genetically Accurate Disease Models with In Silico Analysis to Identify Novel Therapeutic Targets (2016) (48)
Erratum: Control of p70 S6 kinase by kinase activity of FRAP in vivo (Nature (1995) 377 (441-446)) (1995) (48)
Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo. (2016) (47)
Inhibitors of Glycogen Synthase Kinase 3 with Exquisite Kinome-Wide Selectivity and Their Functional Effects. (2016) (47)
Skeletally Diverse Small Molecules Using a Build/Couple/Pair Strategy (2009) (47)
Probing the role of homomeric and heteromeric receptor interactions in TGF-β signaling using small molecule dimerizers (1998) (47)
Stereochemical and Skeletal Diversity Arising from Amino Propargylic Alcohols (2010) (47)
The use of chromatin immunoprecipitation assays in genome-wide analyses of histone modifications. (2004) (47)
Group selective reduction of acetals related to the ansa chain of the streptovaricins: Conformational and stereochemical analysis (1988) (46)
Pathway development and pilot library realization in diversity-oriented synthesis: exploring Ferrier and Pauson-Khand reactions on a glycal template. (2002) (46)
Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria (2011) (46)
Studies relating to the synthesis of the immunosuppressive agent FK-506: coupling of fragments via a stereoselective trisubstituted olefin forming reaction sequence (1989) (45)
DNA-Compatible [3 + 2] Nitrone-Olefin Cycloaddition Suitable for DEL Syntheses. (2018) (45)
The asymmetric epoxidation of divinyl carbinols : theory and applications (1990) (45)
The structure of an HIV-1 specific cell entry inhibitor in complex with the HIV-1 gp41 trimeric core. (2000) (45)
Stereochemistry of the intramolecular enamine/enal (enone) cycloaddition reaction and subsequent transformations (1986) (45)
Chromatin-targeting small molecules cause class-specific transcriptional changes in pancreatic endocrine cells (2012) (44)
A photochemical route to the formation of threo aldols (1983) (44)
Using genome-wide transcriptional profiling to elucidate small-molecule mechanism. (2005) (44)
Diastereotopic selectivity at prochiral carbon centers: functionalization of differentiated hydroxymethyl groups provides access to either stereoisomeric configuration (1985) (44)
Two-directional chain synthesis: the enantioselective preparation of syn-skipped polyol chains from meso precursors (1987) (44)
Distinct binding and cellular properties of synthetic (+)- and (-)-discodermolides. (1994) (44)
Control of olefin geometry in macrocyclic ring-closing metathesis using a removable silyl group. (2011) (44)
On the use of unsymmetrically substituted furans in the furan-carbonyl photocycloaddition reaction: Synthesis of a kadsurenone-ginkgolide hybrid (1988) (43)
An alkynylboronic ester annulation: development of synthetic methods for application to diversity-oriented organic synthesis. (2002) (43)
Integrated genetic and pharmacologic interrogation of rare cancers (2016) (43)
Diversity-oriented organic synthesis and proteomics. New frontiers for chemistry & biology. (2002) (43)
Atomic Structure of the Trypsin-Cyclotheonamide a Complex: Lessons for the Design of Serine Protease Inhibitors (1993) (42)
Studies of the furan-carbonyl photocycloaddition reaction: The determination of the absolute stereostructure of asteltoxin. (1986) (42)
Small-molecule control of insulin and PDGF receptor signaling and the role of membrane attachment (1998) (42)
Progress in Understanding Ferroptosis and Challenges in Its Targeting for Therapeutic Benefit. (2020) (42)
Photo-modulated ion channels based on covalently linked gramicidins. (1991) (42)
Recent achievements and current trajectories of diversity-oriented synthesis. (2020) (42)
Activation of an inactive immunophilin by mutagenesis (1993) (42)
Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia. (2016) (41)
Crystal Structure of P13K SH3 Domain at 2.0 Å Resolution (1996) (41)
Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells. (2017) (41)
Target-based identification of whole-cell active inhibitors of biotin biosynthesis in Mycobacterium tuberculosis. (2015) (41)
Prevention of HIV-1 infection and preservation of CD4 function by the binding of CPFs to gp120. (1990) (41)
Small-Molecule Suppressors of Cytokine-Induced beta-Cell Apoptosis. (2010) (40)
Specific inhibition of formation of transcription complexes by a calicheamicin oligosaccharide: a paradigm for the development of transcriptional antagonists. (1994) (40)
Towards a treatment for genetic prion disease: trials and biomarkers (2020) (40)
Persister cancer cells: Iron addiction and vulnerability to ferroptosis. (2021) (40)
Synthetic investigations of rapamycin. 2. Synthesis of a C(22)-C(42) fragment (1992) (40)
Specific Triggering of the Fas Signal Transduction Pathway in Normal Human Keratinocytes* (1996) (40)
Total synthesis of the anthelmintic agent hikizimycin (1990) (40)
The State of the Art of Chemical Biology (2009) (40)
Revealing complex traits with small molecules and naturally recombinant yeast strains. (2006) (40)
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor (2012) (39)
Molecular Recognition of Immunophilins and Immunophilin-Ligand Complexes (1992) (39)
Studies of the furan-carbonyl photocycloaddition reaction: vinylic substitution reactions (1989) (38)
Exploring the Leucine-Proline Binding Pocket of the Src SH3 Domain Using Structure-Based, Split-Pool Synthesis and Affinity-Based Selection (1998) (37)
Lewis Acid Carbonyl Complexation (1991) (37)
Discovery of Antimalarial Azetidine-2-carbonitriles That Inhibit P. falciparum Dihydroorotate Dehydrogenase (2017) (37)
Proton and nitrogen sequential assignments and secondary structure determination of the human FK506 and rapamycin binding protein. (1991) (37)
Diversity Synthesis of Complex Pyridines Yields a Probe of a Neurotrophic Signaling Pathway (2008) (37)
Characterization of the Prion Protein Binding Properties of Antisense Oligonucleotides (2019) (37)
Identification of a small-molecule inhibitor of class Ia PI3Ks with cell-based screening. (2007) (37)
Identification and structural analysis of residues in the V1 region of CD4 involved in interaction with human immunodeficiency virus envelope glycoprotein gp120 and class II major histocompatibility complex molecules. (1990) (37)
Studies relating to the synthesis of the immunosuppressive agent FK-506: synthesis of the cyclohexyl moiety via a group-selective epoxidation (1989) (36)
Chemical perturbation of an intrinsically disordered region of TFIID distinguishes two modes of transcription initiation (2015) (36)
Synthesis of calcineurin-resistant derivatives of FK506 and selection of compensatory receptors. (2002) (36)
Small-molecule inhibitors directly target CARD9 and mimic its protective variant in inflammatory bowel disease (2017) (36)
Hydrogen transfer from tertiary amines to trifluoroacetic anhydride (1980) (36)
Discovery of Small-Molecule Modulators of the Sonic Hedgehog Pathway (2013) (35)
HDAC6 Inhibitors Modulate Lys49 Acetylation and Membrane Localization of β-Catenin in Human iPSC-Derived Neuronal Cells (2014) (35)
A small-molecule inducer of PDX1 expression identified by high-throughput screening. (2013) (35)
Identification of Inhibitors of PvdQ, an Enzyme Involved in the Synthesis of the Siderophore Pyoverdine (2014) (35)
Studies relating to the synthesis of the immunosuppressive agent FK-506: application of the two-directional chain synthesis strategy to the pyranose moiety (1989) (35)
Specific inhibition of the chymotrypsin-like activity of the proteasome induces a bipolar morphology in neuroblastoma cells. (1996) (34)
Development and Validation of a Novel Leishmania donovani Screening Cascade for High-Throughput Screening Using a Novel Axenic Assay with High Predictivity of Leishmanicidal Intracellular Activity (2015) (34)
Crossing the boundaries (1994) (34)
Aziridines as intermediates in diversity-oriented syntheses of alkaloids. (2009) (34)
Prion protein quantification in human cerebrospinal fluid as a tool for prion disease drug development (2019) (34)
Water-compatible Cycloadditions of Oligonucleotide-conjugated Strained Allenes for DNA-encoded Library Synthesis. (2019) (34)
Modular synthesis and preliminary biological evaluation of stereochemically diverse 1,3-dioxanes. (2004) (34)
Macrocyclic Hedgehog Pathway Inhibitors: Optimization of Cellular Activity and Mode of Action Studies (2012) (33)
AACR Cancer Progress Report 2012 (2012) (33)
Diversity-oriented synthesis yields a new drug lead for treatment of chagas disease. (2014) (33)
Macrocycloadditions leading to conformationally restricted small molecules. (2006) (33)
Synergistic Effects of Stereochemistry and Appendages on the Performance Diversity of a Collection of Synthetic Compounds. (2018) (33)
Structure of the Human 25 kDa FK506 Binding Protein Complexed with Rapamycin (1996) (32)
Discovery of a Small-Molecule Probe for V-ATPase Function (2015) (32)
Immunophilins, ligands, and the control of signal transduction. (1995) (32)
Bicyclic azetidines kill the diarrheal pathogen Cryptosporidium in mice by inhibiting parasite phenylalanyl-tRNA synthetase (2020) (32)
A small molecule suppressor of FK506 that targets the mitochondria and modulates ionic balance in Saccharomyces cerevisiae. (2003) (32)
The Paterno–Büchi Reaction (1991) (32)
Diversity-Oriented Synthesis Probe Targets Plasmodium falciparum Cytochrome b Ubiquinone Reduction Site and Synergizes With Oxidation Site Inhibitors (2014) (31)
Synthesis of chemically reactive analogues of AZT and their biological evaluation against HIV (1988) (31)
Immobilizing the gate of a tartaric acid-gramicidin A hybrid channel molecule by rational design (1990) (31)
KRAS Genomic Status Predicts the Sensitivity of Ovarian Cancer Cells to Decitabine. (2015) (30)
Mapping chemical space using molecular descriptors and chemical genetics: deacetylase inhibitors. (2004) (30)
SpectralNET – an application for spectral graph analysis and visualization (2005) (30)
Identification and characterization of novel sirtuin inhibitor scaffolds. (2009) (30)
Combinatorial Synthesis and Multidimensional NMR Spectroscopy: An Approach to Understanding Protein–Ligand Interactions (1995) (30)
AAK1 identified as an inhibitor of neuregulin-1/ErbB4-dependent neurotrophic factor signaling using integrative chemical genomics and proteomics. (2011) (30)
cDNA cloning of a human 25 kDa FK506 and rapamycin binding protein. (1992) (30)
Synthesis and crystallographic analysis of a bicyclic core related to the esperamicin/calichemicin aglycones (1989) (30)
TGF-β-signaling with small molecule FKBP12 antagonists that bind myristoylated FKBP12-TGF-β type I receptor fusion proteins (1998) (30)
Crystal structures of the selenoprotein glutathione peroxidase 4 in its apo form and in complex with the covalently bound inhibitor ML162. (2021) (30)
Exploiting site-site interactions on solid support to generate dimeric molecules. (2001) (29)
Covalent HLA-B27/peptide complex induced by specific recognition of an aziridine mimic of arginine. (1996) (29)
Iron/copper promoted fragmentation reactions of α-alkoxy hydroperoxides: Regio- and stereocontrolled formation of olefin-containing macrolides (1986) (28)
Diastereoselective control of intramolecular aza-Michael reactions using achiral catalysts. (2011) (28)
Stereochemistry of the 1,2-Wittig rearrangement: A synthesis of syn-1,3-diol monoethers (1987) (28)
Real-Time Biological Annotation of Synthetic Compounds (2016) (28)
Iron/copper promoted fragmentation reactions of .alpha.-alkoxy hydroperoxides. The conversion of octalins into fourteen-membered ring macrolides (1985) (28)
FK506 and rapamycin binding to FKBP: common elements in immunophilin-ligand complexation (1991) (28)
Macrolactones in diversity-oriented synthesis: preparation of a pilot library and exploration of factors controlling macrocyclization. (2004) (28)
A tricyclic ring system replaces the variable regions of peptides presented by three alleles of human MHC class I molecules. (1995) (27)
Diversity-Oriented Synthesis-Facilitated Medicinal Chemistry: Toward the Development of Novel Antimalarial Agents (2014) (27)
Stereospecific Palladium-Catalyzed C-H Arylation of Pyroglutamic Acid Derivatives at the C3 Position Enabled by 8-Aminoquinoline as a Directing Group. (2017) (27)
Histone Variant H2A.Z Marks the 5′ Ends of Both Active and Inactive Genes in Euchromatin (2006) (27)
Further investigations of the type II diels-alder route to the bicyclic core of esperamicin/calichemicin reveal a regiochemical misassignment: Meta vs. para selectivity (1989) (27)
Synthesis and investigations of enetetraynes (1994) (26)
Cell-Specific Calcineurin Inhibition by a Modified Cyclosporin (1997) (26)
Atomic structure of the Immunophilin FKBP13-FK506 Complex: Insights into the Composite Binding Surface for Calcineurin (1994) (26)
Syntheses of stereochemically diverse nine-membered ring-containing biaryls. (2004) (26)
Discovery of Potent and Highly Selective Inhibitors of GSK3b (2014) (26)
Using the Principles of ORGANIC CHEMISTRY to Explore CELL BIOLOGY (1992) (26)
Corrigendum: Selective killing of cancer cells by a small molecule targeting the stress response to ROS (2015) (26)
Renal medullary carcinomas depend upon SMARCB1 loss and are sensitive to proteasome inhibition (2018) (26)
Using High-Throughput Screening Data To Discriminate Compounds with Single-Target Effects from Those with Side Effects (2006) (25)
Synthesis of the angular anthraquinone subunit of dynemicin A (1991) (25)
Identifying cellular targets of small-molecule probes and drugs with biochemical enrichment and SILAC. (2012) (25)
Small-Molecule and CRISPR Screening Converge to Reveal Receptor Tyrosine Kinase Dependencies in Pediatric Rhabdoid Tumors. (2019) (25)
Stereochemical studies of the skipped-polyol polyene macrolide class: Degradation and partial structure determination of mycoticin A and B. (1987) (25)
Revised Structure of the Fungal Germination Self-Inhibitor Gloeosporone (1987) (25)
Mechanisms of immunosuppression by FK506. Preservation of T cell transmembrane signal transduction. (1990) (25)
Identification of Ald6p as the target of a class of small-molecule suppressors of FK506 and their use in network dissection. (2004) (24)
Modular, stereocontrolled Cβ–H/Cα–C activation of alkyl carboxylic acids (2019) (24)
Affinity capillary electrophoresis : insights into the binding of SH3 domains by peptides derived from an SH3-binding protein (1994) (24)
Synthesis of Oxazocenones via Gold(I)-Catalyzed 8-Endo-Dig Hydroalkoxylation of Alkynamides (2015) (24)
Structure-based design of an acyclic ligand that bridges FKBP12 and calcineurin (1993) (24)
STRUCTURAL BASIS FOR PEPTIDOMIMICRY BY A NATURAL PRODUCT (1994) (24)
Synthesis, Structure and Mechanism in Immunophilin Research (1994) (24)
Purification of gramicidin A. (1990) (24)
Small molecule modulation of the human chromatid decatenation checkpoint. (2003) (24)
Synthesis of oxocenones from δ-lactones and their conversion to transposed oxocenes by a reductive Ferrier reaction (1984) (23)
Conformational control of enolate geometry: a short synthesis of germacrene-D (1985) (23)
Kinase-Independent Small-Molecule Inhibition of JAK-STAT Signaling. (2015) (23)
On the preparation of optically active secondary alcohols from a 1,3-dioxan-4-one: Substitution with organocopper reagents (1986) (23)
Expanding Stereochemical and Skeletal Diversity Using Petasis Reactions and 1,3-Dipolar Cycloadditions (2010) (23)
Intramolecular SN' cleavage of allylic ethers by enolate anions (1989) (23)
Distinct effectors of platelet-derived growth factor receptor-alpha signaling are required for cell survival during embryogenesis. (2005) (23)
Ligand design by a combinatorial approach based on modeling and experiment: application to HLA-DR4 (2007) (23)
Type 2 Diabetes Variants Disrupt Function of SLC 16 A 11 through Two Distinct Mechanisms (2017) (23)
Efficient Routes to a Diverse Array of Amino Alcohol-Derived Chiral Fragments (2016) (22)
CTD2 Dashboard: a searchable web interface to connect validated results from the Cancer Target Discovery and Development Network (2017) (22)
Chemical Genetic and Genomic Approaches Reveal a Role for Copper in Specific Gene Activation (1999) (22)
Niche-Based Screening in Multiple Myeloma Identifies a Kinesin-5 Inhibitor with Improved Selectivity over Hematopoietic Progenitors. (2015) (22)
Stereochemical studies of the skipped-polyol polyene macrolide class: NMR studies of a tetraformylal derivative of mycoticin A and B. (1987) (22)
Exploring the Specificity Pockets of Two Homologous SH3 Domains Using Structure-Based, Split-Pool Synthesis and Affinity-Based Selection (1998) (22)
Synthesis and cellular characterization of the detransformation agent, (-)-depudecin. (1995) (22)
Synthetic investigations of rapamycin. 1. Synthesis of a C10-C21 fragment (1992) (22)
Evaluating potential drug targets through human loss-of-function genetic variation (2019) (21)
Synthesis of piperlogs and analysis of their effects on cells. (2013) (21)
Total synthesis of (±)-talaromycin B (1983) (20)
Overproduction of proteins using expression-cassette polymerase chain reaction. (1993) (20)
Overcoming fluconazole resistance in Candida albicans clinical isolates with tetracyclic indoles. (2012) (20)
RWEN: response-weighted elastic net for prediction of chemosensitivity of cancer cell lines (2018) (20)
AN ACID- AND BASE-STABLE O-NITROBENZYL PHOTOLABILE LINKER FOR SOLID PHASE ORGANIC SYNTHESIS (1998) (20)
Global approaches to chromatin. (2002) (20)
Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile. (2016) (20)
Small-molecule control of cytokine function: new opportunities for treating immune disorders. (2014) (20)
Unbiased discovery of in vivo imaging probes through in vitro profiling of nanoparticle libraries. (2009) (20)
Ring-opening and ring-closing reactions of a shikimic acid-derived substrate leading to diverse small molecules. (2007) (19)
Cloning, Zn2+ binding, and structural characterization of the guanine nucleotide exchange factor human Mss4. (1995) (19)
Studies of the immunosuppressive agent FK-506: synthesis of an advanced intermediate (1989) (18)
An FKBP‐Rapamycin‐Sensitive, Cyclin‐Dependent Kinase Activity that Correlates with the FKBP‐Rapamycin‐Induced G1 Arrest Point in MG‐63 Cells a (1993) (18)
Visualizing Functional Group Distribution in Solid-Support Beads by Using Optical Analysis (1999) (18)
Cell-specific transcriptional control of mitochondrial metabolism by TIF1γ drives erythropoiesis (2021) (18)
Synthesis of a bipolar phosphatidylethanolamine: A model compound for a membrane-spanning probe (1987) (18)
Query Chem: a Google-powered web search combining text and chemical structures (2006) (18)
Stereochemical and Conformational Effects on the Cycloaromatization of Dynemicin A-Related Molecules (1995) (18)
BioAssay Research Database (BARD): chemical biology and probe-development enabled by structured metadata and result types (2014) (17)
The NIH's role in accelerating translational sciences (2012) (17)
Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidines (2021) (17)
Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates. (2011) (17)
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells. (2013) (17)
Structure-activity relationships of GPX4 inhibitor warheads. (2020) (17)
Ligand-Enabled β-Methylene C(sp3)-H Arylation of Masked Aliphatic Alcohols. (2020) (17)
Stereochemical studies of simple cyclooctyl systems (1989) (17)
Synthesis of Natural and Modified Trapoxins, Useful Reagents for Exploring Histone Deacetylase Function. (1997) (16)
GW8510 Increases Insulin Expression in Pancreatic Alpha Cells through Activation of p53 Transcriptional Activity (2012) (16)
High-Throughput Screen in Cryptococcus neoformans Identifies a Novel Molecular Scaffold That Inhibits Cell Wall Integrity Pathway Signaling (2015) (16)
Using Expression and Genotype to Predict Drug Response in Yeast (2009) (16)
Diastereotopic selectivity at prochiral carbon centers. A stereodivergent synthesis of the talaromycins (1985) (16)
Allosteric inhibitors of Mycobacterium tuberculosis tryptophan synthase (2020) (16)
A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold. (2011) (16)
Thermodynamic spiroketalization as an efficient method of stereochemical communication (1991) (15)
Diastereotopic group selectivity at a prostereogenic carbon center: Synthesis of (±)-syn-4,8-dimethyldecanal (1986) (15)
Targeting a Therapy-Resistant Cancer Cell State Using Masked Electrophiles as GPX4 Inhibitors (2018) (15)
CHLOROACETAMIDE PHOTOCYCLIZATION OF INDOLE DERIVATIVES. SYNTHESIS, STEREOCHEMISTRY, AND CRYSTAL STRUCTURE OF 3,7-METHANO-3-AZACYCLOUNDECINO(5,4-B)INDOLE (DEETHYLQUEBRACHAMINE) DERIVATIVES (1979) (15)
Protein overproduction for organic chemists (1991) (15)
Stuart Schreiber: biology from a chemist's perspective. Interview by Joanna Owens. (2004) (15)
Identification of Novel Epoxide Inhibitors of Hepatitis C Virus Replication Using a High-Throughput Screen (2007) (15)
ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans (2013) (15)
A Small Molecule Inhibitor of the MITF Molecular Pathway (2014) (15)
Amino Acid Metabolic Origin as an Evolutionary Influence on Protein Sequence in Yeast (2009) (15)
Decoding Products of Diversity Pathways from Stock Solutions Derived from Single Polymeric Macrobeads (2001) (15)
1H and 15N assignments and secondary structure of the PI3K SH3 domain (1993) (15)
Discovery of 8-Membered Ring Sulfonamides as Inhibitors of Oncogenic Mutant Isocitrate Dehydrogenase 1. (2016) (15)
Evolutionarily Conserved Optimization of Amino Acid Biosynthesis (2007) (14)
Ozonolytic Cleavage of Cyclohexene to Terminally Differentiated Products: Methyl 6‐Oxohexanoate, 6,6‐Dimethoxyhexanal, Methyl 6,6‐Dimethoxyhexanoate (2003) (14)
Small-molecule reagents for cellular pull-down experiments. (2008) (14)
An efficient method for the partial synthesis of mixed-chain phosphatidylethanolamines (1987) (14)
The identification and characterization of non-reactive inhibitor of Keap1-Nrf2 interaction through HTS using a fluorescence polarization assay (2013) (13)
Identifying Biologically Active Compound Classes Using Phenotypic Screening Data and Sampling Statistics (2005) (13)
6-Phosphogluconate Dehydrogenase Links Cytosolic Carbohydrate Metabolism to Protein Secretion (2018) (13)
A mercury-catalyzed transetherification cyclization leading to fused cyclic polyethers †,‡ (2000) (13)
Dilazep analogues for the study of equilibrative nucleoside transporters 1 and 2 (ENT1 and ENT2). (2014) (13)
Methylation of Histone H3 K4 Mediates Association of the Isw1p ATPase with Chromatin. (2018) (13)
Disease allele-dependent small-molecule sensitivities in blood cells from monogenic diabetes (2010) (13)
Benzo-fused lactams from a diversity-oriented synthesis (DOS) library as inhibitors of scavenger receptor BI (SR-BI)-mediated lipid uptake. (2015) (13)
Identification of small-molecule inhibitors of Trypansoma cruzi replication. (2011) (13)
SH3 DOMAIN-MEDIATED DIMERIZATION OF AN N-TERMINAL FRAGMENT OF THE PHOSPHATIDYLINOSITOL 3-KINASE p85 SUBUNIT (1994) (13)
Optimization of PDE3A Modulators for SLFN12-Dependent Cancer Cell Killing. (2019) (12)
Automated Structure–Activity Relationship Mining (2014) (12)
Ceestatin, a novel small molecule inhibitor of hepatitis C virus replication, inhibits 3-hydroxy-3-methylglutaryl-coenzyme A synthase. (2011) (12)
Domain-specific Quantification of Prion Protein in Cerebrospinal Fluid by Targeted Mass Spectrometry* (2019) (12)
Transforming Big Data into Cancer-Relevant Insight: An Initial, Multi-Tier Approach to Assess Reproducibility and Relevance (2016) (12)
Barriers to rotation adjacent to double bonds. 5. Remote substituent effects on the syn/skew energy difference for 1-butene (1988) (12)
Total Synthesis of the Immunosuppressive Agent (‐)‐Discodermolide. (1994) (12)
A microarray-based protocol for monitoring the growth of yeast overexpression strains (2006) (12)
CPF-DD is an inhibitor of infection by human immunodeficiency virus and other enveloped viruses in vitro. (1992) (12)
Targeted Protein Degradation by Electrophilic PROTACs that Stereoselectively and Site-Specifically Engage DCAF1. (2022) (11)
Rhabdoid Tumors Are Sensitive to the Protein-Translation Inhibitor Homoharringtonine (2020) (11)
From solution-phase to solid-phase enyne metathesis: crossover in the relative performance of two commonly used ruthenium pre-catalysts. (2005) (11)
Quantitative-Proteomic Comparison of Alpha and Beta Cells to Uncover Novel Targets for Lineage Reprogramming (2014) (11)
Skeletal diversity in small-molecule synthesis using ligand-controlled catalysis. (2007) (11)
Signalling an interest (1994) (11)
A cyclobutene bridgehead olefin approach to the germacranes (1982) (11)
Chromosomal band assignments of the genes encoding human FKBP12 and FKBP13. (1992) (10)
Targeted brachyury degradation disrupts a highly specific autoregulatory program controlling chordoma cell identity (2021) (10)
Differential Pathway Dependency Discovery Associated with Drug Response across Cancer Cell Lines (2017) (10)
Total Synthesis of FK 506 and an FKBP Probe Reagent, (C8, C9-13C2) -FK 506 (1991) (10)
Multilevel regulation of growth rate in yeast revealed using systems biology (2007) (10)
Screen for RAS-Selective Lethal Compounds and VDAC Ligands - Probe 2 (2011) (10)
Apoptosis-inducing natural products found in utero during murine pregnancy. (2000) (10)
TGF-beta-signaling with small molecule FKBP12 antagonists that bind myristoylated FKBP12-TGF-beta type I receptor fusion proteins. (1998) (10)
Enantiomeric Binding Elements Interacting at the Same Site of an SH3 Protein Receptor (1997) (10)
PALP: A rapid imaging technique for stratifying ferroptosis sensitivity in normal and tumor tissues in situ. (2021) (10)
The kinase DYRK 1 A reciprocally regulates the differentiation of Th 17 and regulatory T cells (2015) (10)
Syntheses and discovery of a novel class of cinnamic hydroxamates as histone deacetylase inhibitors by multimodality molecular imaging in living subjects. (2014) (10)
Indolinyl-Thiazole Based Inhibitors of Scavenger Receptor-BI (SR-BI)-Mediated Lipid Transport (2015) (9)
Modulation of ferroptosis sensitivity by TXNRD1 in pancreatic cancer cells (2020) (9)
Diversity‐Oriented Synthesis of Biaryl‐Containing Medium Rings Using a One Bead/One Stock Solution Platform. (2002) (9)
Structure and basicity of silyl ethers: a crystallographic and ab initio inquiry into the nature of silicon-oxygen interactions [Erratum to document cited in CA112(5):35958b] (1990) (9)
Cyclobutene bridgehead olefin route to the American cockroach sex pheromone, periplanone-B (2002) (9)
pCyP B: A Cyclophilin Chloroplast-Localized, Heat Shock- Responsive from Fava Bean (1994) (9)
Computational repurposing of therapeutic small molecules from cancer to pulmonary hypertension (2021) (9)
High Throughput Screen Identifies Interferon γ-Dependent Inhibitors of Toxoplasma gondii Growth. (2018) (9)
An Asymmetric Synthesis of (+)-Cryptone (1990) (9)
Selective inhibitors of SARM1 targeting an allosteric cysteine in the autoregulatory ARM domain (2022) (9)
Multimodal small-molecule screening for human prion protein binders (2020) (8)
Discovery of bisamide-heterocycles as inhibitors of scavenger receptor BI (SR-BI)-mediated lipid uptake. (2015) (8)
Identification of a small molecule that selectively inhibits alpha-synuclein translational expression (2011) (8)
HIF-2α drives an intrinsic vulnerability to ferroptosis in clear cell renal cell carcinoma (2018) (8)
Divergent Synthesis and Real-Time Biological Annotation of Optically Active Tetrahydrocyclopenta[c]pyranone Derivatives (2016) (8)
Identification of a small molecule inhibitor of Pseudomonas aeruginosa PvdQ acylase, an enzyme involved in siderophore pyoverdine synthesis (2013) (8)
ReviewDeacetylase Enzymes : Biological Functions and the Use of Small-Molecule Inhibitors (2002) (8)
Whole Genome Amplification by T7-Based Linear Amplification of DNA (TLAD): Overview. (2008) (8)
Exploring the Specificity Pockets of Two Homologous SH3 Domains Using Structure‐Based, Split‐Pool Synthesis and Affinity‐Based Selection. (1998) (7)
Forward Chemical Genetics (2008) (7)
The interaction of CD4 with HIV-1 gp120. (1991) (7)
Control of Olefin Geometry in Macrocyclic Ring‐Closing Metathesis Using a Removable Silyl Group. (2011) (7)
Quantifying fitness distributions and phenotypic relationships in recombinant yeast populations (2007) (7)
Reactions That Proceed with a Combination of Enantiotopic Group and Diastereotopic Face Selectivity Can Deliver Products with Very High Enantiomeric Excess: Experimental Support of a Mathematical Model. (1987) (6)
Domain-specific Quantification of Prion Protein in Cerebrospinal Fluid by Targeted Mass Spectrometry. (2019) (6)
Erratum to ‘Dissecting cellular processes using small molecules: identification of colchicine-like, taxol-like and other small molecules that perturb mitosis’: [Chem. Biol. 7 (2000) 275-286] (2001) (6)
Identification of Small Molecule Inhibitors that Suppress Cytokine-Induced Apoptosis in Human Pancreatic Islet Cells (2011) (6)
The conformation of cyclosporin a bound to cyclophilin is altered (once again) following binding to calcineurin: an analysis of receptor-ligand-receptor interactions (1992) (6)
The promise and peril of chemical probes (vol 11, pg 536, 2015) (2015) (6)
Retraction Note: Selective killing of cancer cells by a small molecule targeting the stress response to ROS (2018) (6)
Reassignment of Stereochemistry and Total Synthesis of the Thrombin Inhibitor Cyclotheonamide B. (1992) (6)
Discovery of Inhibitors of Anti-Apoptotic Protein A1 (2011) (6)
Whole Genome Amplification by T7-Based Linear Amplification of DNA (TLAD): II. Second-Strand Synthesis and In Vitro Transcription. (2008) (6)
Stereochemical Diversity as a Source of Discovery in Chemical Biology (2022) (6)
Total Synthesis of FK506 and an FKBP Probe Reagent, (C8,C9-13C2)-FK506. (1990) (5)
Chemical genetics identifies small-molecule modulators of neuritogenesis involving neuregulin-1/ErbB4 signaling. (2010) (5)
Chemoproteomics quantifies complexity (2011) (5)
Crystallization-Based Synthetic Route to Antimalarial Agent BRD5018: Diazocene Ring Formation via a Staudinger-aza-Wittig Reaction on an Azetidine-Ribose Template (2021) (5)
Prion protein quantification in cerebrospinal fluid as a tool for prion disease drug development (2018) (5)
Is there a scaffolding domain within the structure of the immunosuppressive agent cyclosporin a (CsA)? Studies of the cyclophilin binding domain of CsA (1988) (5)
Corrigendum: The promise and peril of chemical probes. (2015) (5)
Automated Structure-Activity Relationship Mining: Connecting Chemical Structure to Biological Profiles (2016) (5)
Relationship of FKBP to PKCI-2 (1991) (5)
Rethinking relationships between natural products. (2007) (4)
Molecular Design of Transmembrane Ion Channels (1991) (4)
FKBP, thought to be identical to PKCI-2, does not inhibit protein kinase C (1991) (4)
Protein Kinases as Targets in Cancer Therapy: Validated and Emerging Approaches (2005) (4)
ML238: An Antimalarial Small Molecule of a Unique Structural Class (2011) (4)
A Small Molecule Inhibitor of Scavenger Receptor BI-mediated Lipid Uptake—Probe 1 (2014) (4)
ReviewIntegration of Growth Factor and Nutrient Signaling : Implications for Cancer (2003) (4)
Total Synthesis of (-)-Hikizimycin Employing the Strategy of Two-Directional Chain Synthesis. (1992) (4)
Synthesis and Analysis of 506BD, a High‐Affinity Ligand for the Immunophilin FKBP. (1992) (4)
A new journal for an expanding field (1994) (4)
Identification of Small Molecules that Selectively Inhibit Fluconazole-Resistant Candida Albicans in the Presence of Fluconazole but not in its Absence - Probe 3 (2011) (4)
Gene Expression-Based Screen for Parkinson's Disease Identifies GW8510 as a Neuroprotective Agent. (2016) (4)
Syntheses of Aminoalcohol‐Derived Macrocycles Leading to a Small‐Molecule Binder to and Inhibitors of Sonic Hedgehog. (2010) (4)
Erratum: The promise and peril of chemical probes (Nature Chemical Biology (2015) 11 (536-541)) (2015) (4)
Novel quaternary structures of the human prion protein globular domain. (2021) (4)
Study of receptor-ligand interactions through receptor labeling and isotope-edited NMR (1991) (4)
Syntheses of Stereochemically Diverse Nine‐Membered Ring‐Containing Biaryls. (2005) (3)
Whole Genome Amplification by T7-Based Linear Amplification of DNA (TLAD): III. Sample Purification. (2008) (3)
The transcriptional profile of Saccharomyces cerevisiae exposed to rapamycin mimics the profile induced by amino acid starvation (1999) (3)
The Use of Informer Sets in Screening: Perspectives on an Efficient Strategy to Identify New Probes (2021) (3)
[19] – Overproduction of Proteins Using Expression-Cassette Polymerase Chain Reaction (1995) (3)
A Soft-Drug Histone Deacetylase Inhibitor for Cutaneous T-Cell Lymphoma. (2007) (3)
A Small Molecule Inhibitor of Scavenger Receptor BI-mediated Lipid Uptake—Probe 2 (2014) (3)
Discovering Small Molecules that Overcome Differentiation Arrest in Acute Myeloid Leukemia (2015) (3)
Structural and Synthetic Studies of the Spore Germination Autoinhibitor Gloeosporone. (1988) (3)
Bicyclic azetidines target acute and chronic stages of Toxoplasma gondii by inhibiting parasite phenylalanyl t-RNA synthetase (2022) (3)
(2 + 2) PHOTOCYCLOADDITIONS IN THE SYNTHESIS OF CHIRAL MOLECULES (1985) (3)
Modular Synthesis of Cyclopropane-Fused N-Heterocycles Enabled by Underexplored Diazo Reagents. (2022) (3)
Chapter 11 - Total Synthesis of the FK506/FKBP Complex (1991) (3)
antitumor activity in multiple myeloma Small-molecule inhibition of proteasome and aggresome function induces synergistic (2005) (3)
Crystallization and preliminary X-ray analysis of twinned crystals of a chimeric FK506 binding protein 12 and 13 complexed with FK506. (1996) (3)
Whole Genome Amplification by T7-Based Linear Amplification of DNA (TLAD): I. CIP Treatment of Samples and Tailing Reaction with Terminal Transferase. (2008) (3)
Chemical Genetic Analysis of Platelet Granule Secretion-Probe 2 (2011) (3)
Rationales Design neuer Rezeptor‐Ligand‐Kombinationen (1995) (3)
Stereochemistry of the Intramolecular Enamine/Enal (Enone) Cycloaddition Reaction and Subsequent Transformations. (1987) (3)
Inhibition of T-Cell Signaling (2005) (3)
Transannular Diels-Alder Route to Systems Related to Dynemicin A. (2010) (2)
Catalytic Asymmetric [3 + 2] Cycloaddition of Azomethine Ylides. Development of a Versatile Stepwise, Three‐Component Reaction for Diversity‐Oriented Synthesis. (2003) (2)
FRAGMENTATION REACTIONS OF α-ALKOXY HYDROPEROXIDES AND APPLICATION TO THE SYNTHESIS OF THE MACROLIDE (.+-.)-RECIFEIOLIDE (1980) (2)
Proteomic discovery of chemical probes that perturb protein complexes in human cells (2022) (2)
US immigration order strikes against biotech (2017) (2)
Cobalt-Mediated Total Synthesis of (+)-Epoxydictymene. (1994) (2)
Discovery and Evaluation of Fungicidal Anti-Cryptococcal Molecules (2015) (2)
Identification of Small-Molecule Inhibitors of Trypansoma cruzi Infection - Probe 3 (2011) (2)
A Small Molecule Inhibitor of Scavenger Receptor BI-mediated Lipid Uptake - Probe 3 (2013) (2)
Inhibition of Plasmodium falciparum phenylalanine tRNA synthetase provides opportunity for antimalarial drug development. (2022) (2)
The Asymmetric Epoxidation of Divinyl Carbinols: Theory and Applications. (1990) (2)
Screen for Inhibitors of STK33 Kinase Activity (2014) (2)
N‐Oxide‐Promoted Pauson‐Khand Cyclizations at Room Temperature. (1991) (2)
Total Syntheses of Di- and Tri-O-methyl Dynemicin A Methyl Esters. (1994) (2)
Synthesis, Structure, and Mechanism in Immunophilin Research (1995) (2)
Identification of Small-Molecule Inhibitors of Trypansoma cruzi Infection - Probe 1 (2011) (2)
Author Correction: Cytochrome P450 oxidoreductase contributes to phospholipid peroxidation in ferroptosis (2021) (1)
Two‐Directional Chain Synthesis: An Application to the Synthesis of (+) ‐Mycoticin A. (1993) (1)
Conformational Control of Enolate Geometry: A Short Synthesis of Germacrene-D. (1986) (1)
Structural Insight into Allosteric Inhibition of Mycobacterium tuberculosis Tryptophan Synthase (2017) (1)
Niche-Based Screening Reveals Leukemia Stem Cell Specific Therapeutics (2011) (1)
DNA-encoded library (DEL)-enabled discovery of proximity-inducing small molecules (2022) (1)
Therapeutics , Targets , and Chemical Biology Integrative Radiogenomic Pro fi ling of Squamous Cell Lung Cancer (2013) (1)
Opposite Patterns of Synchrony in Sympatric Disease Metapopulations (1999) (1)
Corrigendum: Large-scale chemical dissection of mitochondrial function (2008) (1)
A Candidate Cell-Selective Anticancer Agent (2014) (1)
Neocarzinostatin activation: molecular modeling revisited (1994) (1)
Type 2 Diabetes‐Associated Variants Disrupt Function of SLC16A11, a Proton‐Coupled Monocarboxylate Transporter, Through Two Distinct Mechanisms (2017) (1)
π-Bond Hybridization in Transition Metal Complexes (1991) (1)
TOTAL SYNTHESIS OF (.+-.)-ASTELTOXIN (1984) (1)
An Asymmetric Synthesis of (+)-Cryptone (I). (1990) (1)
Cover Picture: Expanding the Functional Group Compatibility of Small-Molecule Microarrays: Discovery of Novel Calmodulin Ligands (Angew. Chem. Int. Ed. 21/2003) (2003) (1)
Total Synthesis of (‐)‐Rapamycin Using an Evans‐Tishchenko Fragment Coupling. (1993) (1)
Author Correction: Evaluating drug targets through human loss-of-function genetic variation (2021) (1)
Lenalidomide Promotes CRBN-Mediated Ubiquitination and Degradation of IKZF1 and IKZF3 (2013) (1)
Total Synthesis of the Anthelmintic Agent Hikizimycin. (1991) (1)
Discovery of ML370, an inhibitor of Vibrio cholerae Quorum Sensing Acting via the LuxO response regulator (2014) (1)
Novel quaternary structures of the human prion protein globular domain (2020) (1)
Integrative Radiogenomic Profiling Identifies BRAF Mutations as Novel Radiotherapeutic Targets in Adenocarcinomas of the Lung (2014) (1)
Syntheses of α-Pyrones Using Gold-Catalyzed Coupling Reactions. (2011) (1)
1 High-Throughput Screening Identifies Small-Molecule Enhancers of 2 Reactive Oxygen Species That are Nontoxic or Cause Genotype- 3 Selective Cell Death (2013) (1)
Application of the Allylic Diazene Rearrangement: Synthesis of the Enediyne‐Bridged Tricyclic Core of Dynemicin A. (1992) (1)
Epoxidation of Unsaturated Macrolides: Stereocontrolled Routes to Ionophore Subunits. (1986) (1)
Discovery of Two, Structurally Distinct Agonists of Vibrio cholerae Quorum Sensing Acting via the CqsS Membrane Receptor (2013) (1)
A Signaling Pathway to Minireview Translational Control (1996) (1)
IRON/COPPER PROMOTED FRAGMENTATION REACTIONS OF α-ALKOXY HYDROPEROXIDES. THE CONVERSION OF OCTALINS INTO FOURTEEN-MEMBERED RING MACROLIDES (1985) (1)
PALP: An imaging method for detecting and quantifying polyunsaturated phospholipids via peroxidation (2020) (1)
Disrupting fluconazole resistance in Candida albicans clinical isolates with tetracyclic indoles (2013) (1)
Niche-Based Screening Identifies Novel Small Molecules That Overcome Stromal Effects in Multiple Myeloma (2012) (1)
Discovery of small molecule probe that shows anti-tubercular activity via Mtb bioA (DAPA synthase) enzyme inhibition (2015) (1)
Correction: GW8510 Increases Insulin Expression in Pancreatic Alpha Cells through Activation of p53 Transcriptional Activity (2012) (1)
Chemistry and Biology of the Immunophilins and Their Immunosuppressive Ligands (1991) (1)
Synthetic Studies in the Brefeldin Series: Asymmetric Enamine‐Enal Cycloaddition and Intramolecular Nozaki Reactions. (1988) (0)
Figure 4, PHI inhibitors lacking a carboxylic acid (2013) (0)
Figure 56, Spectroscopic data for SID 99376537 (2012) (0)
APPLICATION OF THE FURAN CARBONYL PHOTOCYCLADDITION REACTION TO THE SYNTHESIS OF THE BIS(TETRAHYDROFURAN) MOIETY OF ASTELTOXIN (1984) (0)
Syntheses of Discodermolides Useful for Investigating Microtubule Binding and Stabilization. (1997) (0)
Abstract 2985: DNA-damage related histone marks can distinguish the anti-tumor effects of established and novel histone deacetylase inhibitors in ovarian cancer cells (2010) (0)
Figure 26, Spectroscopic data for SID 99376527 (2012) (0)
Abstract B17: Identification of Druggable Targets through Functional Multi-Omics in Renal Medullary Carcinoma (2017) (0)
Iron/Copper Promoted Fragmentation Reactions of a-Alkoxy Hydroperoxides: Regio- and Stereocontrolled Formation of Olefin-Containing Macrolides. (1986) (0)
Figure 6, Dose-dependent Activity of the Probe (ML280) (2014) (0)
INTRAMOLECULAR ITK-PROLINE COMPLEX, NMR, MINIMIZED AVERAGE STRUCTURE (1998) (0)
Regulated intracellular association of proteins using cell-permeable synthetic ligands (1994) (0)
Figure 4, Heat Map Comparisons of Differential Gene Expression (2013) (0)
Figure 5, ML316 Selectively Inhibits Growth of C. albicans (A and B) over 3T3 Fibroblasts (C) (2014) (0)
Abstract 3026: Targeting GPX4 in tumor-associated stromal cells increases inflammatory-cell infiltration (2017) (0)
Table 4, Percent Inhibition of Selected Kinases by HTS Hit (CID 5706819) at 10 μM (2014) (0)
Figure 2, STK33 Inhibitors (2014) (0)
Figure 4, Probe Stability in PBS solution at 23 °C (2012) (0)
Table 4, Comparison of Breast Cancer Stem Cells: Probes 1, 2, and 3 (2013) (0)
Structure oftheFKBP12-Rapamycin ComplexInteracting withtheBinding DomainofHumanFRAP (2016) (0)
mammalian three-hybrid screen Inducible gene expression and protein translocation using nontoxic ligands identified by a (2006) (0)
Figure 4, Dose Response Curves for Initial Hit, MLS000888573 (2014) (0)
Table 6, Substituted aliphatic amine analogsa (2013) (0)
Figure 8, Summary of analogs prepared to investigate the SAR profile of hit CID 665390 (2014) (0)
Figure 30, Spectroscopic data for SID 99376511 (2012) (0)
Figure 38, Spectroscopic data for SID 99376525 (2012) (0)
1980s Camelot (2019) (0)
Figure 16, Spectroscopic data for SID 99376520 (2012) (0)
Table 7, Substituted benzyl amine analogsa (2013) (0)
Figure 23, Spectroscopic data for SID 99376531 (2012) (0)
Figure 1B, Stability of Probe (ML312) to GSH (with 1% DMSO) (2013) (0)
Crystal structure of human dihydroorotate dehydrogenase at 1.7 A resolution (2016) (0)
Plasmodium vivax cytoplasmic Phenylalanyl-tRNA synthetase in complex with BRD1389 (2020) (0)
C-SRC SH3 DOMAIN COMPLEXED WITH LIGAND APP12 (1996) (0)
Table 1, Summary of Assays Completed (2012) (0)
Figure 3, Stability of ML280 in PBS Buffer (pH 7.4, 23ºC) over 48 Hours (2014) (0)
Table 11, SAR of the Benzylic Position (2014) (0)
Table 1, Summary of Probe (ML318) Properties Computed from Structure (2013) (0)
Figure 18, Spectroscopic data for SID 99376522 (2012) (0)
Figure 43, Spectroscopic data for SID 99376518 (2012) (0)
Synthesis of a Bipolar Phosphatidylethanolamine: A Model Compound for a Membrane-Spanning Probe. (1987) (0)
Table 1, Summary of Known Probe (ML280) Properties in PubChem (2014) (0)
Discovery of a Small Molecule Activator of the Hypoxia Inducible Factor Pathway (2013) (0)
Crystal structure of human dihydroorotate dehydrogenase with ML390 (2016) (0)
Author response: The kinase DYRK1A reciprocally regulates the differentiation of Th17 and regulatory T cells (2015) (0)
Figure 7, Known Inhibitors Against GSK3 (2014) (0)
Design and Characterization of a Novel, Reverse Prodrug Histone Deacetylase Inhibitor for Cutaneous T-Cell Lymphoma. (2006) (0)
Chemical Perturbation of an Intrinsically Disordered Region of TFIID Distinguishes de novo Transcription Initiation from Reinitiation (2016) (0)
Figure 6, Compound screening process (critical path) (2013) (0)
Conformation and Structure of Organometal Complexes in the Solid State: Two Important Studies to Understand Chemical Reactions (1990) (0)
Functional Profiling of a Glioblastoma (GBM) Patient-Derived Cell Line (PDCL) Panel Identifies Cell-Intrinsic Differential Radiation Response That Correlates With TP53 Mutations (2015) (0)
Figure 5, Dose Response Curves for initial hit (CID 665390) and optimized probe (CID 70680248) (2014) (0)
Figure 3, Heat Map Comparisons of Differential Gene Expression (2013) (0)
Figure 9, Dose response curves of probe and analogs submitted to SMR collection in primary assay (2013) (0)
Figure 60, Spectroscopic data for SID 99245570 (2012) (0)
Figure 33, Spectroscopic data for SID 99245557 (2012) (0)
Figure 3, Small molecules targeting non-replicating Mtb in different stress condition (2015) (0)
Table 8, SAR of Heteroaromatic Replacements of Phenyl Group (2014) (0)
Scheme 1, Synthesis of the Probe (CID49843203/ML239) (2013) (0)
Figure 1A, Stability of Probe (ML312) in PBS Buffer (with 1% DMSO, pH 7.4, 23°C) (2013) (0)
Global Nucleosome Occupancy in Yeast The Harvard community has made this article openly available. Please share how this access benefits you. Your story matters (2004) (0)
Studies of the Furan‐Carbonyl Photocycloaddition Reaction: The Determination of the Absolute Stereostructure of Asteltoxin. (1986) (0)
Pathway Development and Pilot Library Realization in Diversity‐Oriented Synthesis. Exploring Ferrier and Pauson—Khand Reactions on a Glycal Template (2003) (0)
Abstract B11: Targeting mesenchymal cells in the tumor stroma by GPX4 inhibition (2016) (0)
Stereospecific Total Synthesis of (.+-.)-Cafestol. Total Synthesis of (.+-.)-Atractyligenin (1989) (0)
SYNTHETIC STUDIES OF THE FURAN-CARBONYL PHOTOCYCLOADDITION REACTION. A TOTAL SYNTHESIS OF (.+-.)-AVENACIOLIDE (1985) (0)
Abstract 4974: Pharmacogenomic interactions in glioblastoma cell line models (2017) (0)
Scheme 1, Synthesis of Probe (CID53377439/ML278) (2014) (0)
Figure 39, Spectroscopic data for SID 99376508 (2012) (0)
Figure 37, Spectroscopic data for SID 99376512 (2012) (0)
Synthesis and HDAC Inhibitory Activity of Largazole Analogs: Alteration of the Zinc-Binding Domain and Macrocyclic Scaffold (2009) (0)
THE STRUCTURE OF THE IMMUNOPHILIN-IMMUNOSUPPRESSANT FKBP12-RAPAMYCIN COMPLEX INTERACTING WITH HUMAN FRAP (1997) (0)
Table 14, Absolute Selectivity of Selected Compounds (2014) (0)
Abstract NG13: Metabolomic adaptations and correlates of survival to immune checkpoint blockade (2020) (0)
Figure 7, Dose-dependent Activity of the Probe (ML281) (2014) (0)
Systematic Investigation of Genetic Vulnerabilities Across Cancer Cell Lines Reveals Lineage Specific Radiotherapeutic Determinants (2015) (0)
Table 3, SAR of the Phenyl Group (ortho-substitution) (2014) (0)
Validation of Chordoma Cell Lines (2015) (0)
[Figure, Probe Structure and Characteristics]. (2010) (0)
Scheme 1, Synthesis of Probe 3 (ML312) (2013) (0)
New method of identifying and examining molecules with bilogica activity. (1995) (0)
Abstract PR15: Functional analysis of diverse oncogenic driver mutations using an isogenic cell line library identifies novel drug responses and alterations in metabolism (2015) (0)
Figure 6, Heat Map Comparisons of Differential Gene Expression by ML245 and CID50904149 (2014) (0)
Peptides antiviraux a terminaisons bloquees (1991) (0)
Table 9, Physical Properties of Substituted Quinoline Analogs (2012) (0)
The rise of molecular glues and bifunctional compounds (2022) (0)
Complex alpha-pyrones synthesized by a gold-catalyzed coupling reaction. (2007) (0)
Figure 10, Summary of SAR Performed on the Thiazolone Scaffold (52 analogs, 52S) (2014) (0)
Studies on the Furan-Carbonyl Photocycloaddition Reaction: Vinylic Substitution Reactions. (1990) (0)
An Efficient Method for the Partial Synthesis of Mixed-Chain Phosphatidylethanolamines (I). (1987) (0)
Figure 42, Spectroscopic data for SID 99376530 (2012) (0)
Figure 44, Spectroscopic data for SID 99376526 (2012) (0)
Table 3, Prior Art Substance Identifiers (2013) (0)
Figure 54, Spectroscopic data for SID 99376503 (2012) (0)
Figure 13, Best-in-class Chemosensitizers for Reversing Fluconazole Resistance (MIC=1.2–2.8 μM) (2012) (0)
Table 4, SAR in the isoxazole seriesa (2013) (0)
Scheme 1, Synthesis of the Probe (ML320) (2014) (0)
Conference Report : Chemical Synthesis and Drug Discovery : ICS Symposium Honoring (2016) (0)
Figure 4, Known Small Molecules Inhibitors of Breast Cancer Stem Cells (2013) (0)
Figure 11, Summary of the SAR on the Quinoxalinone Scaffold (40 analogs, 40S) (2014) (0)
Abstract 4596: An integrated genomic characterization of the target of a small molecule identifies a novel cancer dependency (2014) (0)
Towards Diversity-Oriented Stereoselective Syntheses of Biaryl- or Bis(aryl)metal-Containing Medium Rings. (2000) (0)
Figure 34, Spectroscopic data for SID 99245539 (2012) (0)
Table 8, SAR Analysis on the Eastern Ring: Influence of Heterocycles (2014) (0)
Figure 31, Spectroscopic data for SID 99245553 (2012) (0)
Table 12, SAR with the CF3-pyrazole (2014) (0)
Table 16, Selectivity Data Versus Aurora B for Selected Quinoxalinone Analogs (2014) (0)
Table 3, Comparison of the Probe (ML243) to Project Criteria (2013) (0)
HOMOLOGOUS DOMAIN OF HUMAN FKBP25 (1996) (0)
MB-103DiSCoVERing INNOVATIVE THERAPIES: COMBINING GENETICALLY ACCURATE DISEASE MODELS OF MEDULLOBLASTOMA WITH ADVANCED IN SILICO ANALYSIS TO IDENTIFY NOVEL THERAPEUTIC TARGETS (2016) (0)
Macrocycloadditions leading to conformationally restricted small molecules (Organic Letters (2006) 8 (2065)) (2009) (0)
CCDC 816668: Experimental Crystal Structure Determination (2011) (0)
CRIEGEE REARRANGEMENT OF α-ALKOXY HYDROPEROXIDES. A SYNTHESIS OF ESTERS AND LACTONES THAT COMPLEMENTS THE BAEYER-VILLIGER OXIDATION OF KETONES (1983) (0)
Small-molecule targeting of brachyury transcription factor addiction in chordoma (2019) (0)
Figure 1, Stability Data for the Probe (CID 49835877/ML239) in PBS Plus Acetonitrile Over 48 Hours (2013) (0)
Table 17, Comparison of the Probe to Project Criteria (2014) (0)
Table 12, SAR Analysis on the Northern Ring: Amides (2014) (0)
Scheme 1, Synthesis of Probe ML370 (2014) (0)
Table 7, SAR Analysis on the Eastern Ring: Influence of Halogen Substituents (2014) (0)
Abstract 2476: DiSCoVERing innovative therapies for rare tumors: Combining genetically accurate disease models with advanced in silico analysis to identify novel therapeutic targets (2016) (0)
Target- and Diversity-Oriented Organic Synthesis in Drug Discovery (2000) (0)
Table 9, Probe Activation of Quorum Sensing in Vibrio cholerae Mutant Strains (2014) (0)
Figure 61, Spectroscopic data for SID 99376515 (2012) (0)
Figure 1, Reported Inhibitors of SR-BI (2014) (0)
Title: KRAS genomic status predicts the sensitivity of ovarian cancer cells to decitabine Running Title: KRAS status predicts sensitivity to decitabine in ovarian cancer Authors: Stewart ML, Tamayo (2015) (0)
Table 4, Evaluation of Additional Amides and Amide Bond Surrogates (2012) (0)
Revised Structure of the Fungal Germination Self‐Inhibitor Gloeosporone. (1987) (0)
Figure 3, Critical Path for Probe Development (2014) (0)
Table 7, Structural Modifications of the Acyl Group (2014) (0)
Table 7, Physical Properties of Piperazine Derivatives (2012) (0)
Figure 21, Spectroscopic data for SID 99376507 (2012) (0)
Titelbild: Expanding the Functional Group Compatibility of Small‐Molecule Microarrays: Discovery of Novel Calmodulin Ligands (Angew. Chem. 21/2003) (2003) (0)
Targeted genes regulated by the transcription and other biological functions (1995) (0)
The two complementary methods of understanding a transcription profile (2011) (0)
Figure 5, Known Small Molecules Inhibitors of Breast Cancer Stem Cells (2013) (0)
New method for detection and evaluation of biologically active molecules (1995) (0)
Figure 36, Spectroscopic data for SID 99245548 (2012) (0)
ROS induction as a strategy to target persister cancer cells with low metabolic activity in NRAS mutated melanoma (2022) (0)
Figure D1, ORTEP Rendition of Intermediate 7 (2014) (0)
Abstract 1953: Accelerating prediction of pediatric and rare cancer vulnerabilities using next-generation cancer models (2017) (0)
Scheme 1, Synthesis of the Probe ML408 (2015) (0)
2010 JBS/SBS Academic Excellence Awards (2010) (0)
Table 2, Solubility of ML370 and Analogs in PBS and LB Media (2014) (0)
Diversity-Oriented Syntheses Using the Build / Couple / Pair Strategy * * (2011) (0)
Abstract B077: Comprehensive molecular characterization and high-throughput chemical screening identifies genetic dependencies and molecular vulnerabilities in glioblastoma cell line models (2018) (0)
Synthesis and Investigations of Enetetraynes. (2010) (0)
Figure 5, Percent of Kinome Inhibited by CHIR99021 and Three New Compounds (2014) (0)
Inhibiteurs bifonctionnels d'histone déacétylase (2007) (0)
Abstract 4259: The radiogenomic landscape of cancer (2014) (0)
Table 10, SAR of the pyrazole (2014) (0)
Tandem Use of Cobalt-Mediated Reactions to Synthesize (+)- Epoxydictymene, a Diterpene Containing a trans-Fused 5-5 Ring System. (1997) (0)
Table 2, Compounds submitted to the SMR Collection (2013) (0)
An Alkynylboronic Ester Annulation: Development of Synthetic Methods for Application to Diversity‐Oriented Organic Synthesis. (2003) (0)
Thermodynamic Spiroketalizations as an Efficient Method for Stereochemical Communication. (1992) (0)
Diversity-oriented synthesis encoded by deoxyoligonucleotides (2023) (0)
Figure 4, Stability of Probe ML370 in 1:1 Acetonitrile:PBS (pH 7.4, 23 °C) (2014) (0)
On the Use of Unsymmetrically Substituted Furans in the Furan-Carbonyl Photocycloaddition Reaction: Synthesis of a Kadsurenone-Ginkgolide Hybrid. (1989) (0)
Figure 46, Spectroscopic data for SID 99376513 (2012) (0)
Scheme 2, Synthesis of Probe ML281 (2014) (0)
Figure 25, Spectroscopic data for SID 99376504 (2012) (0)
The landscape of cancer cell line metabolism (2019) (0)
Figure 1, Stability of the Probe (ML334) in PBS Buffer (pH 7.4, 23°C) (2013) (0)
Figure 15, Spectroscopic data for SID 99245531 (2012) (0)
22(I-8) Diversity-Oriented Synthesis of Indole Alkaloids (2004) (0)
Table 2, Data from Additional Assays (2013) (0)
MIPALRELGS ATPEEYNTW QKPRQILCQF IDRILTDVNV VAVELVKKTD SQPTSVMLLD FIQHIMKSSP LMFVNVSGSH EAKGSCIEFS NWIITRLLRI AATPSCHLLH KKICEVICSL LFLFKSKSPA IFGVLTKELL QLFEDLVYLH RRNVMGHAVE WPWMSRFLS QLDEHMGYLQ SAPLQLMSMQ NLEFIEVTLL MVLTRIIAIV FFRRQELLLW QIGCVLLEYG SPKIKSLAIS FLTELFQLGG LPAQPASTFF SSFLELLKHL VEMDT (2005) (0)
Table 5, Physical Properties of Additional Amides and Amide Bond Surrogates (2012) (0)
Figure 3, Comparison of ML312 to Prior Art Compounds with DiI-HDL Uptake (2013) (0)
Probing Metabolic Requirements for Fungal Virulence — Probe 1 (2014) (0)
Abstract PR07: Functional analysis of diverse oncogenic driver mutations using an isogenic cell line library identifies novel drug responses and alterations in metabolism (2015) (0)
Figure 32, Spectroscopic data for SID 99376523 (2012) (0)
Synthesis of the Bicyclic Core of the Esperamicin/Calichemicin Class of Antitumor Agents. (1988) (0)
Figure 4, Dose-dependent Activity of Select Analogs in the Primary Assay (2014) (0)
Table 1, Calculated Property Comparison of ML228 with MDDR Compounds (2013) (0)
Intramolecular SN′ Cleavage of Allylic Ethers by Enolate Anions. (1989) (0)
Combinatorial Synthesis and Multi-Dimensional NMR Spectroscopy - An Understanding of Protein-Ligand Interactions (1995) (0)
Figure 3, 2-Oxoglutarate (2-OG) and PHD inhibitor analogs (2013) (0)
Abstract PR04: Integration of CRISPR-Cas9, RNAi and pharmacologic screens identify actionable targets in a rare cancer (2016) (0)
Table 6, Structural Modifications of the Core Region (2014) (0)
Figure 3, Dose Inhibition Assay of HMLE_shGFP, HMLE_shECad, and HMLE_shTwist by the Probe (ML243) (2013) (0)
Asymmetric Alkynylation of Isoquinoline Iminium Salts (2006) (0)
Figure 9, Profiling of ML280 and ML281 against a panel of 83 kinases (2014) (0)
Abstract B13: Human pancreatic cancer organoids for functional dependency profiling (2016) (0)
Treatment of solid tumors (2006) (0)
Figure 53, Spectroscopic data for SID 99376524 (2012) (0)
Application of the Two-Directional Chain Synthesis Strategy to the First Stereochemical Assignment of Structure to Members of the Skipped-Polyol Polyene Macrolide Class: Mycoticin A and B. (1988) (0)
Figure 40, Spectroscopic data for SID 99376517 (2012) (0)
Table 2, Summary of Probe Properties Computed from Structure ML316 (2014) (0)
Table 1, Summary of Probe Properties from PubChem* (2014) (0)
Diastereotopic Group Selectivity at a Prostereogenic Carbon Center: Synthesis of (.+-.)-syn-4,8-Dimethyldecanal. (1987) (0)
Evaluating drug targets through human loss-of-function genetic variation (2020) (0)
Table 2, SAR of the Amide (2014) (0)
Table 10, Heteroaromatic Substitution of the 7-chloroquinoline (2012) (0)
Acceleration of the Dess-Martin Oxidation by Water. (1995) (0)
Figure 5, STK-33 Kinase Screening Funnel (2014) (0)
Figure 1, The Endogenous Ligand of the Vibrio cholerae Sensor Histidine Kinase CqsS, Cholera autoinducer-1 (CAI-1) (2014) (0)
Discovery and Characterization of Small Molecule Inhibitors of Autophagy for Cancer Therapy. (2006) (0)
Abstract A103: High-throughput genomic and chemical screening in glioblastoma cell lines. (2013) (0)
Towards a patient-based drug discovery (2012) (0)
Proposed Resolution of a Mechanistic Puzzle of Long Duration: Self-Condensation of Cyclopentanone to Form an 11-Carbon Dienoic Acid. (2023) (0)
3 p Relocation Mediates a Transcriptional Response to Rapamycin in Yeast repression (2004) (0)
Bicyclic azetidines target acute and chronic stages of Toxoplasma gondii by inhibiting parasite phenylalanyl t-RNA synthetase (2022) (0)
Stereochemical and Conformational Effects on the Cycloaromatization of Dynemicin A‐Related Molecules (1995) (0)
Table 8, Lead Profiler results with ML228 at 10 μM (2013) (0)
Abstract 2028: PDE3A modulation for cancer therapy (2017) (0)
Crystal structure of tryptophan synthase from M. tuberculosis - ligand-free form, TrpA-G66V mutant (2017) (0)
Figure 6, SAR Summary (2014) (0)
Table 3, Probe attributes (2014) (0)
Abstract 181: Therapeutic approaches to metastasis induced by mesenchymal stem cells in the tumor microenvironment (2014) (0)
Table 3, Liver Microsome Stability of the Probe ML408 (CID 72725758) and CID 780674 (2015) (0)
STRUCTURE OF SIGNAL TRANSDUCTION PROTEIN, NMR, MINIMIZED AVERAGE STRUCTURE (1997) (0)
The Radiogenomic Landscape of Cancer (2014) (0)
Abstract B38: Developing a functional genomics platform to interrogate rare pediatric cancers (2016) (0)
Table 5, Analysis of the HTS Hit Compound (2014) (0)
Table 3, Physical Properties of 4-chlorobenzamide Derivatives (2012) (0)
Figure 14, Spectroscopic data for SID 99245537 (2012) (0)
102(P-52) Pathway Development for Library Realization on Carbohydrate and Steroidal Scaffolds by Diversity-Oriented Organic Synthesis (2002) (0)
Figure 1, Stability of the Probe (ML408, CID 72725758) in PBS Buffer (pH 7.4, 23 °C) (2015) (0)
Table 5, PubChem Assays Reporting Dose-Dependent Activity of CID 665390 (the hit compound)* (2014) (0)
Table 2, Summary of SAR Performed Upon the 4-chlorobenzamide (2012) (0)
Figure 62, Spectroscopic data for SID 99376533 (2012) (0)
Stereochemistry of the 1,2-Wittig Rearrangement: A Synthesis of syn-1,3-Diol Monoethers. (1987) (0)
Figure 45, Spectroscopic data for SID 99245559 (2012) (0)
Proximity and orientation underlie signaling by the non-receptor tyrosine kinase ZAP 70 of myristoylation was to bring the src-like tyrosine kinases (2013) (0)
Preclinical Development of a Novel Antimalarial Agent (2019) (0)
Natural Products as a Probe of Cellular Functions: Studies of Immunophilins (2010) (0)
Abstract IA1: Cancer dependencies defined by genomic alterations and targeted by small molecules (2012) (0)
Figure 47, Spectroscopic data for SID 99376519 (2012) (0)
Figure 35, Spectroscopic data for SID 99245543 (2012) (0)
Figure 10, Shape based molecular graphics aligned with the SurflexSim and conformational ensemble illustrate the large dissimilarity in shape and volume of the probe compound ML228 (greensurface, capped sticks) with the composite shape of the J&J PHD2 ligands (white surface) (2013) (0)
Small-molecule and CRISPR screening converge to reveal RTK dependencies in pediatric rhabdoid tumors (2020) (0)
Identification and Characterization of Novel Small-Molecule Inhibitors of the Replication Checkpoint. (2004) (0)
Table 3, Hits of interest following cherry pick CRCs (2013) (0)
Figure 7, Heat Map Comparisons of Differential Gene Expression by Salinomycin (2014) (0)
Figure 4, a) Ribbon diagram depicting GSK3b and CID 5524264 in the ATP binding pocket b) Surface representation showing the binding site, binding orientation and absolute configuration of CID 5524264 (2014) (0)
Figure 1, Stability Data for the Probe (ML243) in PBS Buffer (pH 7.4, 23°C) Plus Acetonitrile over 48 Hours (2013) (0)
Chinese scientists and US leadership in the life sciences (2019) (0)
Figure 4, Activity profile of TCA1 in carbon starvation assay (2015) (0)
Table 14, SAR Analysis on the Eastern Ring (2014) (0)
Table 6, Biological Assay of Piperazine Derivatives (2012) (0)
Figure 2, General iron chelator desferrioxamine (DFO) (2013) (0)
Figure 57, Spectroscopic data for SID 99376553 (2012) (0)
2021 – TRANSCRIPTIONAL REGULATION OF MITOCHONDRIAL METABOLISM BY TIF1GAMMA DRIVES ERYTHROID PROGENITOR DIFFERENTIATION (2020) (0)
Table 3, SAR Analysis of Ethyl Carbamate (2014) (0)
A precision oncology approach to the pharmacological targeting of mechanistic dependencies in neuroendocrine tumors (2018) (0)
High-Throughput Screening of Novel Heat Shock Protein 90 (Hsp90) and Histone Deacetylase (HDAC) Inhibitors through Molecular Imaging of Hsp90/Co-chaperone p23 Interactions in Living Subjects (2007) (0)
SOLUTION STRUCTURE OF HUMAN MSS4, A GUANINE NUCLEOTIDE EXCHANGE FACTOR FOR RAB PROTEINS (2000) (0)
Table 11, Physical Properties of the Heteroaromatic Surrogates (2012) (0)
Table 10, SAR Analysis on the Western Phenyl Ring (2014) (0)
Table 6, SAR of Alkyl Replacements of Phenyl Group (2014) (0)
Abstract IA25: Linking genetic features of human cancers and histone-modifying enzymes for future cancer therapies (2013) (0)
Figure 8, Future Medicinal Chemistry Plans (2014) (0)
Structure–activity Relationships of Glutathione Peroxidase 4 Inhibitor Warheads (2020) (0)
Targeting the Protein Degradation Pathway in Multiple Myeloma with Synergistic, Selective Small Molecules. (2005) (0)
Elucidation of the physiology of non-replicating, drug tolerant Mycobacterium tuberculosis with the aid of the small molecule probe ML338 (2013) (0)
Figure 17, Spectroscopic data for SID 99376521 (2012) (0)
Crystal structure of tryptophan synthase from M. tuberculosis - BRD4592-bound form (2017) (0)
Solid-Phase Enyne Metathesis Using Ruthenium Pre-catalysts (2005) (0)
Chemical Biology Towards Precision Medicine (2017) (0)
Figure 3, Electrophilic Keap1 inhibitors (2013) (0)
Table 19, Comparison of the probes to reported STK33 inhibitors (2014) (0)
ReviewGlobal Approaches to Chromatin A third area in which systematic approaches are yield - (2002) (0)
Figure 19, Spectroscopic data for SID 99376499 (2012) (0)
π-Bond Hybridization in Transition-Metal Complexes. A Stereoelectronic Model for Conformational Analysis (1991) (0)
Prion protein quantification in cerebrospinal fluid as a tool for prion disease therapeutic development (2019) (0)
Table 1, Comparison of the Probe (ML239) to Project Criteria (2013) (0)
Table 11, Selectivity Data Versus Aurora B for Selected Thiazolone Analogs (2014) (0)
Dynamic Behavior of Dicobalt Hexacarbonyl Propargyl Cations and Their Reactions with Chiral Nucleophiles. (1988) (0)
Figure 1, Some known inhibitors of fungal mitochondria oxidative phosphorylation (2014) (0)
Abstract ND04: BAY 2666605: The first PDE3A-SLFN12 complex inducer for cancer therapy (2022) (0)
Figure 8, Effect of ML280 and ML281 on KRAS dependent (Red) and independent (Blue) cell-line viability (2014) (0)
Figure 29, Spectroscopic data for SID 99376510 (2012) (0)
Figure 2, Recovery of Undissolved Probe (ML278) from PBS Buffer (pH 7.4, 23 °C) (2014) (0)
A GPX4-dependent cancer cell state underlies the clear-cell morphology and confers sensitivity to ferroptosis (2019) (0)
Table 9, SAR of the A ring (2014) (0)
Table 8, Comparison of New & Existing Cholera QS Probes to Project Criteria (2014) (0)
Synthesis of Chemically Reactive Analogues (I) of AZT and Their Biological Evaluation Against HIV. (1988) (0)
Figure 9, Possible Directions for Future SAR Investigation of ML370 (2014) (0)
A j3-lactone related to lactacystin induces neurite outgrowth in a neuroblastoma cell line and inhibits cell cycle progression in an osteosarcoma cell line (0)
Table 2, Microsomal Stability of Select Compounds (2014) (0)
Table 7, SAR of Mono-Substitution on the Phenyl Group (2014) (0)
Abstract 4367: Accelerating prediction of tumor vulnerabilities using next-generation cancer models (2016) (0)
On the Preparation of Optically Active Secondary Alcohols from a 1,3-Dioxan-4-one: Substitution with Organocopper Reagents. (1986) (0)
Abstract B26: Accelerating prediction of tumor vulnerabilities using next-generation cancer models (2016) (0)
Figure 3, Aza-uracil-derived antagonists of LuxO ATPase activity (2014) (0)
Table 1, Summary of Probe Properties Computed from Structure ML408 (2015) (0)
Abstract LB216: Targeted brachyury degradation disrupts a highly specific autoregulatory program controlling chordoma cell identity (2021) (0)
Pik-related kinases in the response to DNA damage by UV (1998) (0)
Structure of Mycobacterium tuberculosis tryptophan synthase: a model system for allosteric inhibition (2017) (0)
Abstract B48: Identification of novel drug interactions with MYC via a quantitative chemical-genetic interaction map (2015) (0)
A Mercury‐Catalyzed Transetherification Cyclization Leading to Fused Cyclic Polyethers. (2001) (0)
Table 13, Potency of Enantiomers (2014) (0)
DIASTEREOTOPICGROUPSELECTIVITYATAPROSTEREOGENICCARBONCENTER: SYNTHESIS OF(?)-SYN-4,fbDIMETHYLDECANAL (1986) (0)
Figure 27, Spectroscopic data for SID 99245535 (2012) (0)
Reference compounds for characterizing cellular injury in high-content cellular morphology assays (2022) (0)
Figure 4, Dose response curves of probe and analogs submitted to SMR collection (2013) (0)
Identification of a chemically validated target in replicating and non-replicating Mycobacterium tuberculosis with the aid of a small molecule probe (2015) (0)
A Boronic Ester Annulation Strategy for Diversity‐Oriented Organic Synthesis. (2002) (0)
Abstract C136: Identification of selective cancer cytotoxic modulators of phosphodiesterase 3a by predictive chemogenomics (2015) (0)
Scheme 1, Synthesis of the Probe (ML212) (2013) (0)
Figure 28, Spectroscopic data for SID 99376509 (2012) (0)
Figure 58, Spectroscopic data for SID 99376545 (2012) (0)
Total Synthesis of FK 506 and an FKBP Probe Reagent, (C8,C9-13C2)-FK 506. Chemistry and Biology of the Immunophilins and Their Immunosuppressive Ligands (1992) (0)
Table 3, PubChem bioassays in which the ML280 screening hits were active (2014) (0)
Figure 41, Spectroscopic data for SID 99376498 (2012) (0)
Table 5, Initial SAR in the triazine seriesa (2013) (0)
Abstract PR04: Transcriptional regulation of mitochondrial metabolism by TIF1γ drives erythroid progenitor differentiation (2020) (0)
Plasticity of ether lipids promotes ferroptosis susceptibility and evasion (2020) (0)
Utility of Histone deacetylase 6, a novel estrogen regulated gene affecting cell motility, as predictive factor for adjuvant endocrine treatment and as therapeutic target (2005) (0)
CHAPTER 7 DNA linear amplification (2005) (0)
Figure 55, Spectroscopic data for SID 99376554 (2012) (0)
Retraction Note: Selective killing of cancer cells by a small molecule targeting the stress response to ROS (2018) (0)
Abstract 1520: Identifying differential dependency networks accounting for response to NEDD8-inhibitor in large-scale cancer cell line data (2016) (0)
Functional profiling of a glioblastoma (GBM) patient-derived cell line (PDCL) panel to identify cell-intrinsic differential radiation response. (2016) (0)
Abstract 3315: Functional genomic profiling of lung adenocarcinoma identifies BRAF mutations as novel therapeutic targets (2015) (0)
Figure 7, Complete dose response curves for probe (ML228, CID 46742353, SID 98626463) (2013) (0)
Synthesis of skeletally diverse β-lactam haptens for the in vitro diagnosis of IgE-mediated drug allergy. (2022) (0)
Scheme 1, Synthesis of Probe ML280 (2014) (0)
Abstract C88: Genomics, advocacy, and emerging therapeutics to address triple-negative breast cancer (TNBC) outcome disparities. (2016) (0)
Abstract SY42-01: Chemical biology-based approach to understanding and overcoming resistance of cancers to therapies (2019) (0)
TOTAL SYNTHESIS OF (.+-.)-TALAROMYCIN B (1984) (0)
Table 13, SAR Analysis on the Northern Ring: Amines and Sulfonamides (2014) (0)
Scheme 3, Synthetic strategy employed to explore SAR on the northern portion of the hit (2014) (0)
High throughput screen identifies IFN-γ-dependent inhibitors of Toxoplasma gondii growth (2018) (0)
Figure 22, Spectroscopic data for SID 99245567 (2012) (0)
Autophagy as a Target Pathway in Multiple Myeloma: A Forward Chemical Genetic Approach. (2007) (0)
Traitement de troubles lies a la degradation de proteines (2006) (0)
Enantiospecific Total Synthesis of the Protein Phosphatase Inhibitor Motuporin (IX). (1995) (0)
Figure 10, Evaluating Loss of C. glabrata Mitochondrial Membrane Potential with JC-1 (2014) (0)
1980s Camelot (2019) (0)
Figure 10, Critical Path (2012) (0)
Figure 51, Spectroscopic data for SID 99245561 (2012) (0)
Author Correction: Evaluating drug targets through human loss-of-function genetic variation (2021) (0)
Table 4, Summary of Probe Properties Computed for ML370 (2014) (0)
Table 5, Thiazolone Hit Compounds (2014) (0)
Figure 2, Dose Response Curves for the Probe (ML312) (2013) (0)
Figure 1, Stability of Probe (ML318) in PBS Buffer (pH 7.4, 23°C) (2013) (0)
Figure 4, Stability of the Probe (ML281) in PBS Buffer (pH 7.4, 23 ºC) over 48 Hours (2014) (0)
Figure 2, The V cholerae CqsS/CAI-1 Quorum Sensing Phosphorelay system (2014) (0)
Figure 3, Dose-dependent Activity of the Probe (ML320) in Target (GSK3b, left) and Anti- Target (CDK5, right) (2014) (0)
Abstract 2313: DDR1 receptor kinase pathway as an emerging target in cancer therapeutics (2011) (0)
Figure 50, Spectroscopic data for SID 99376557 (2012) (0)
Table 1, Summary of Known Probe Properties in PubChem* (2014) (0)
Figure 1, RAS Synthetic Lethal Compounds Against Targets Discovered Through RNAi Screens (2014) (0)
Esperamicins, a Novel Class of Potent Antitumor Antibiotics. Part 2 and 3. Calichemicins, a Novel Family of Antitumor Antibiotics. Part 1 and 2 (1989) (0)
Table 1, Plasma Stability of Probe ML316 and analogs CID3889161 and CID56604835 (2014) (0)
Modular Synthesis of Cyclopropane‐Fused N‐Heterocycles Enabled by Underexplored Diazo Reagents (2022) (0)
Table 15, Comparison of Activity and Physical Properties of CHIR99021 and ML320 (2014) (0)
Table 2, Comparison of Probes to Select Prior Art Compounds (2013) (0)
Table 1, Strains of V. cholera used in assays (2014) (0)
Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidines (2021) (0)
Abstract B44: A systems approach combining genomics, advocacy, and emerging novel therapeutics to address triple-negative breast cancer (TNBC) outcomes disparities (2015) (0)
Figure 52, Spectroscopic data for SID 99245569 (2012) (0)
Figure 1, Stability Data for the Probe (ML320) in PBS Buffer (pH 7.4, 23°C) followed by addition of acetonitrile after 48 Hours (2014) (0)
Mapping the landscape of genetic dependencies in chordoma (2022) (0)
Build/couple/pair strategy: From nonchiral molecules to unbiased scaffolds, a methodological approach for the optimization of microwave-assisted intra-molecular Diels-Alder reaction of furans (2008) (0)
Figure 1, HIF-1α regulation in response to oxygen availability (2013) (0)
Figure 24, Spectroscopic data for SID 99376500 (2012) (0)
Figure 5, Comparison of Probe to Prior Art Compounds (2013) (0)
Identiﬁcation of Novel Epoxide Inhibitors of Hepatitis C Virus Replication Using a High-Throughput Screen (cid:1) †§ (2007) (0)
Table 16, Comparison of CHIR 99021 Kinase profile and ML320 (% Inhibition at 10 μM) (2014) (0)
Two-Directional Chain Synthesis: The Enantioselective Preparation of syn-Skipped Polyol Chains from Meso Precursors. (1987) (0)
Figure 5, Johnson and Johnson benzimidazole PHD inhibitors (2013) (0)
Figure 5, Dose Inhibition Assay of HMLE_sh_GFP, HMLE_sh_ECad, and HMLE_sh_Twist by the Probe (ML245) (2014) (0)
Figure 11, Manual docking of ML228 positioned to chelate iron in the active site to a structural overlay of PHD2 ligand bound J&J structures reveals a sterically constrained site (2013) (0)
Histone Deacetylase-6 (HDAC6) Modulates Akt and STAT3 Activity Via Heat Shock Protein (Hsp) 90 in Human Multiple Myeloma (MM) Cells. (2006) (0)
Table 3, Thiol Stability (DTT) and Plasma Stability for ML370 (2014) (0)
Table 8, Summary of SAR Performed with Substituted Quinolines (2012) (0)
Figure 59, Spectroscopic data for SID 99376552 (2012) (0)
GATING PHENOMENA IN COVALENTLY LINKED GRAMICIDIN CHANNELS (1990) (0)
Figure 48, Spectroscopic data for SID 99376502 (2012) (0)
Scheme D1, Synthesis of the Amgen Compound 1 (control) (2014) (0)
Figure 8, Complete dose response curves (continued) for probe (ML228: CID 46742353) (2013) (0)
Figure 2, Dose-dependent Activity of the Probe (ML239) in Target and Counterscreen Assays (2013) (0)
Beth Levine in memoriam (2020) (0)
Abstract B098: GPX4 is a broadly shared gene vulnerability among residual tumors (2018) (0)
Table 1, Summary of Known Probe (ML312) Properties Computed from Structure (2013) (0)
Table 15, SAR Analysis on the Southern Ring (2014) (0)
Figure 3, Dose-dependent activity of the probe (ML318) (2013) (0)
Figure 49, Spectroscopic data for SID 99376538 (2012) (0)
Figure 2, Dose-dependent Activity of the Probe (ML334) (2013) (0)
Table 2, Plasma Stability and Plasma Protein Binding of ML408 (CID 72725758) and CID 780674 (2015) (0)
Figure 20, Spectroscopic data for SID 99376501 (2012) (0)
Table 2, Summary of Known Probe (ML281) Properties in PubChem (2014) (0)
Chemical Biology Intervention in Cells Based on Chemical Principles (2013) (0)
ROS Induction Targets Persister Cancer Cells with Low Metabolic Activity in NRAS-Mutated Melanoma. (2023) (0)
Abstract A02: Expanding tumor chemical-genetic interaction map using next-generation cancer models (2017) (0)

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