Craig M. Crews
American professor of molecular biology
Craig M. Crews's AcademicInfluence.com Rankings

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Biology
Why Is Craig M. Crews Influential?
(Suggest an Edit or Addition)According to Wikipedia, Craig M. Crews is an American scientist at Yale University. He is the John C. Malone Professor of Molecular, Cellular, and Developmental Biology, and also holds joint appointments in the departments of Chemistry and Pharmacology. Crews is the Executive Director of the Yale Center for Molecular Discovery and a former Editor of the journal Cell Chemical Biology. His research interests focus on chemical biology, particularly on controlled proteostasis. Crews is a pioneer in the field of targeted protein degradation and his lab's research led to the development of the anti-cancer drug carfilzomib . He is the founder of Arvinas, the first biotechnology company to bring PROTAC drugs into clinical trials. In 2019, he was named an American Cancer Society Research Professor at the Yale University.
Craig M. Crews's Published Works
Published Works
- Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradation (2001) (1083)
- Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity. (1999) (925)
- The primary structure of MEK, a protein kinase that phosphorylates the ERK gene product. (1992) (892)
- Induced protein degradation: an emerging drug discovery paradigm (2016) (768)
- Catalytic in vivo protein knockdown by small-molecule PROTACs. (2015) (709)
- Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. (2015) (683)
- The anti-angiogenic agent fumagillin covalently binds and inhibits the methionine aminopeptidase, MetAP-2. (1997) (577)
- Molecular Understanding and Modern Application of Traditional Medicines: Triumphs and Trials (2007) (503)
- PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer (2016) (494)
- The anti-inflammatory natural product parthenolide from the medicinal herb Feverfew directly binds to and inhibits IkappaB kinase. (2001) (461)
- The ubiquitin‐proteasome pathway and proteasome inhibitors (2001) (419)
- Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead. (2017) (418)
- Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL. (2016) (401)
- Structure of human methionine aminopeptidase-2 complexed with fumagillin. (1998) (393)
- Extracellular signals and reversible protein phosphorylation: What to Mek of it all (1993) (392)
- Small-Molecule PROTACS: New Approaches to Protein Degradation. (2016) (387)
- Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery (2020) (386)
- Targeted protein degradation: expanding the toolbox (2019) (381)
- Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics. (2008) (340)
- PROteolysis TArgeting Chimeras (PROTACs) - Past, present and future. (2019) (338)
- PROTAC targeted protein degraders: the past is prologue (2022) (337)
- Chemical genetic control of protein levels: selective in vivo targeted degradation. (2004) (329)
- The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. (2017) (319)
- Targeting the von Hippel–Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1α Interaction (2012) (309)
- Selective inhibitors of the osteoblast proteasome stimulate bone formation in vivo and in vitro. (2003) (298)
- Targeted protein degradation by PROTACs☆ (2017) (288)
- Small-Molecule Hydrophobic Tagging Induced Degradation of HaloTag Fusion Proteins (2011) (264)
- Crystal Structure of Epoxomicin:20S Proteasome reveals a molecular basis for selectivity of alpha,beta-Epoxyketone Proteasome Inhibitors (2000) (261)
- Development of Protacs to Target Cancer-promoting Proteins for Ubiquitination and Degradation* (2003) (254)
- Targeted protein degradation: elements of PROTAC design. (2019) (246)
- HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins. (2015) (245)
- Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase (2019) (245)
- Reconstitution of the Raf-1—MEK—ERK Signal Transduction Pathway In Vitro (1993) (242)
- Triptolide is a traditional Chinese medicine-derived inhibitor of polycystic kidney disease (2007) (227)
- Targeted Protein Degradation: from Chemical Biology to Drug Discovery. (2017) (225)
- A genetic interaction network of five genes for human polycystic kidney and liver diseases defines polycystin-1 as the central determinant of cyst formation (2011) (216)
- Purification of a murine protein-tyrosine/threonine kinase that phosphorylates and activates the Erk-1 gene product: relationship to the fission yeast byr1 gene product. (1992) (200)
- Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance (2018) (197)
- Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation. (2018) (196)
- Total synthesis of the potent proteasome inhibitor epoxomicin: a useful tool for understanding proteasome biology. (1999) (178)
- Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α. (2012) (175)
- Waste disposal—An attractive strategy for cancer therapy (2017) (170)
- Small-Molecule Modulation of Protein Homeostasis. (2017) (163)
- Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation. (2018) (157)
- PROTACs: An Emerging Therapeutic Modality in Precision Medicine. (2020) (156)
- Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1. (2017) (155)
- Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs (2020) (154)
- Interleukin 2 stimulation of p70 S6 kinase activity is inhibited by the immunosuppressant rapamycin. (1992) (152)
- Proteolysis-Targeting Chimeras: Induced Protein Degradation as a Therapeutic Strategy. (2017) (150)
- Eponemycin exerts its antitumor effect through the inhibition of proteasome function. (1999) (149)
- MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53. (2018) (146)
- Dissecting fragment-based lead discovery at the von Hippel-Lindau protein:hypoxia inducible factor 1α protein-protein interface. (2012) (143)
- Sequence and expression of chicken and mouse rsk: homologs of Xenopus laevis ribosomal S6 kinase (1989) (143)
- Pharmacological Targeting of the Pseudokinase Her3 (2014) (141)
- Targeting steroid hormone receptors for ubiquitination and degradation in breast and prostate cancer (2008) (138)
- Towards subunit-specific proteasome inhibitors: synthesis and evaluation of peptide α', β'-epoxyketones (1999) (137)
- Novel BET protein Proteolysis Targeting Chimera (BET-PROTAC) exerts superior lethal activity than Bromodomain Inhibitor (BETi) against post-myeloproliferative Neoplasm (MPN) Secondary (s) AML Cells (2016) (133)
- Erks: their fifteen minutes has arrived. (1992) (129)
- Design and Applications of Bifunctional Small Molecules: Why Two Heads Are Better Than One. (2008) (128)
- The Selective Proteasome Inhibitors Lactacystin and Epoxomicin Can Be Used to Either Up- or Down-Regulate Antigen Presentation at Nontoxic Doses1 (2000) (125)
- Lack of proteasome active site allostery as revealed by subunit-specific inhibitors. (2001) (124)
- Total synthesis of TMC-95A and -B via a new reaction leading to Z-enamides. Some preliminary findings as to SAR. (2004) (124)
- Small-Molecule-Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging. (2015) (124)
- Reversible Spatiotemporal Control of Induced Protein Degradation by Bistable PhotoPROTACs (2019) (123)
- The antiangiogenic agent TNP-470 requires p53 and p21CIP/WAF for endothelial cell growth arrest. (2000) (118)
- Small-molecule control of intracellular protein levels through modulation of the ubiquitin proteasome system. (2014) (118)
- From epoxomicin to carfilzomib: chemistry, biology, and medical outcomes. (2013) (117)
- Chemical genetics: exploring and controlling cellular processes with chemical probes. (1999) (111)
- GTP-dependent binding of the antiproliferative agent didemnin to elongation factor 1 alpha. (1994) (110)
- BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cells (2018) (110)
- Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency. (1999) (109)
- Targeted Protein Degradation by Small Molecules. (2017) (109)
- Raf-1 forms a stable complex with Mek1 and activates Mek1 by serine phosphorylation. (1993) (108)
- Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs (2013) (105)
- Targeting the undruggable proteome: the small molecules of my dreams. (2010) (100)
- Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation. (2017) (99)
- Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion. (2018) (94)
- Highly efficient targeted mutagenesis in axolotl using Cas9 RNA-guided nuclease (2014) (93)
- Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation. (2019) (93)
- Cells adapted to the proteasome inhibitor 4-hydroxy- 5-iodo-3-nitrophenylacetyl-Leu-Leu-leucinal-vinyl sulfone require enzymatically active proteasomes for continued survival. (2001) (92)
- Phorbol ester stimulates a protein-tyrosine/threonine kinase that phosphorylates and activates the Erk-1 gene product. (1992) (91)
- Proteasome inhibition by fellutamide B induces nerve growth factor synthesis. (2008) (89)
- The Proteasome in Modern Drug Discovery: Second Life of a Highly Valuable Drug Target (2017) (88)
- Triptolide reduces cystogenesis in a model of ADPKD. (2008) (82)
- Mouse Erk-1 gene product is a serine/threonine protein kinase that has the potential to phosphorylate tyrosine. (1991) (81)
- Wound epidermis formation and function in urodele amphibian limb regeneration. (2008) (79)
- A chemical and genetic approach to the mode of action of fumagillin. (2006) (78)
- Total synthesis and structure-activity investigation of the marine natural product neopeltolide. (2009) (72)
- Targeted protein knockdown using small molecule degraders. (2017) (71)
- Major advances in targeted protein degradation: PROTACs, LYTACs, and MADTACs (2021) (70)
- ARV-110: An oral androgen receptor PROTAC degrader for prostate cancer. (2019) (70)
- Activation of the planar cell polarity formin DAAM1 leads to inhibition of endothelial cell proliferation, migration, and angiogenesis (2010) (69)
- A role for planar cell polarity signaling in angiogenesis (2008) (68)
- Targeted protein degradation: a promise for undruggable proteins. (2021) (65)
- MEK2 is a kinase related to MEK1 and is differentially expressed in murine tissues. (1993) (64)
- Identification of Hydrophobic Tags for the Degradation of Stabilized Proteins (2012) (62)
- Gene expression profile of the regeneration epithelium during axolotl limb regeneration (2011) (62)
- Targeted Protein Destabilization Reveals an Estrogen-mediated ER Stress Response (2014) (61)
- Chemical genetics: adding to the developmental biology toolbox. (2003) (61)
- Chemical Inducers of Targeted Protein Degradation* (2010) (59)
- Eponemycin analogues: syntheses and use as probes of angiogenesis. (1998) (59)
- Triptolide reduces cyst formation in a neonatal to adult transition Pkd1 model of ADPKD. (2010) (59)
- Chemical biology: Greasy tags for protein removal (2012) (58)
- Protein Targeting Chimeric Molecules Specific for Bromodomain and Extra-terminal Motif Family Proteins are Active Against Pre-Clinical Models of Multiple Myeloma (2018) (57)
- Small-molecule inhibitors of the cell cycle. (2000) (56)
- Molecular and Cellular Basis of Regeneration and Tissue Repair (2007) (56)
- Targeted gene disruption of methionine aminopeptidase 2 results in an embryonic gastrulation defect and endothelial cell growth arrest (2006) (56)
- Proteolysis-Targeting Chimeras: Harnessing the Ubiquitin-Proteasome System to Induce Degradation of Specific Target Proteins (2018) (56)
- Targeted Degradation of Transcription Factors by TRAFTACs: Transcription Factor Targeting Chimeras (2020) (55)
- RUNX1 targeted therapy for AML expressing somatic or germline mutation in RUNX1. (2019) (55)
- Abstract P5-04-18: ARV-471, an oral estrogen receptor PROTAC degrader for breast cancer (2019) (54)
- Recent Developments in PROTAC‐Mediated Protein Degradation: From Bench to Clinic (2021) (53)
- Triptolide-induced transcriptional arrest is associated with changes in nuclear substructure. (2008) (52)
- Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties. (2019) (51)
- Didemnin binds to the protein palmitoyl thioesterase responsible for infantile neuronal ceroid lipofuscinosis. (1996) (49)
- Mutant-selective degradation by BRAF-targeting PROTACs (2020) (47)
- Synthesis of 9-fluorenylmethoxycarbonyl-protected amino aldehydes (1998) (47)
- Studies on calcium dependence reveal multiple modes of action for triptolide. (2005) (46)
- Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation (2021) (44)
- Development of small molecules targeting the pseudokinase Her3. (2015) (44)
- Triptolide Directly Inhibits dCTP Pyrophosphatase (2011) (43)
- Feeding the machine: mechanisms of proteasome-catalyzed degradation of ubiquitinated proteins. (2003) (39)
- Microarray Analysis of microRNA Expression during Axolotl Limb Regeneration (2012) (39)
- Synthetic studies on amphidinolide B1. (2006) (36)
- BETP degradation simultaneously targets acute myelogenous leukemia stem cells and the microenvironment. (2019) (36)
- PROTACs: past, present and future. (2022) (35)
- Towards subunit-specific proteasome inhibitors: synthesis and evaluation of peptide alpha',beta'-epoxyketones. (1999) (35)
- Total synthesis and biological evaluation of tyroscherin. (2010) (35)
- An oral androgen receptor PROTAC degrader for prostate cancer. (2017) (32)
- The antiproliferative agent didemnin B uncompetitively inhibits palmitoyl protein thioesterase. (1998) (32)
- Neurotrophic peptide aldehydes: solid phase synthesis of fellutamide B and a simplified analog. (2006) (30)
- Chemical Approaches to Controlling Intracellular Protein Degradation (2005) (29)
- Disruption of Wnt planar cell polarity signaling by aberrant accumulation of the MetAP-2 substrate Rab37. (2011) (29)
- Targeting nuclear β-catenin as therapy for post-myeloproliferative neoplasm secondary AML (2018) (28)
- Stereoselective assembly of a 1,3-diene via coupling between an allenic acetate and a (B)-alkylborane: synthetic studies on amphidinolide B1. (2005) (28)
- A bidirectional system for the dynamic small molecule control of intracellular fusion proteins. (2013) (26)
- Development and characterization of proteasome inhibitors. (2005) (26)
- Abstract 5236: ARV-110: An androgen receptor PROTAC degrader for prostate cancer (2018) (26)
- Simplified Synthetic TMC‐95A/B Analogues Retain the Potency of Proteasome Inhibitory Activity (2003) (26)
- Lineage tracing of genome-edited alleles reveals high fidelity axolotl limb regeneration (2017) (25)
- Developing microcolin A analogs as biological probes. (2005) (25)
- Targeted protein unfolding uncovers a Golgi-specific transcriptional stress response (2018) (23)
- Inducing Protein Degradation as a Therapeutic Strategy. (2016) (23)
- Inducing Protein Degradation as a Therapeutic Strategy. (2018) (23)
- Total synthesis of luminacin D. (2002) (22)
- Synthesis of the C3-C18 fragment of amphidinolides G and H. (2007) (21)
- Natural product inhibitors of the ubiquitin-proteasome pathway. (2011) (20)
- A Single Amino Acid Residue Defines the Difference in Ovalicin Sensitivity between Type I and II Methionine Aminopeptidases* (2004) (20)
- Targeted Protein Internalization and Degradation by ENDosome TArgeting Chimeras (ENDTACs) (2019) (20)
- Protein folding state-dependent sorting at the Golgi apparatus (2019) (20)
- Modulation of Phosphoprotein Activity by Phosphorylation Targeting Chimeras (PhosTACs). (2021) (19)
- Efficient Synthesis of Immunomodulatory Drug Analogues Enables Exploration of Structure–Degradation Relationships (2018) (19)
- Chemical genetics: exploring the role of the proteasome in cell biology using natural products and other small molecule proteasome inhibitors. (2008) (19)
- Efficient stereoselective syntheses of isopanepoxydone and panepoxydone: a re-assignment of relative configuration (2000) (18)
- Small-molecule inhibitors of the cell cycle: an overview. (2003) (17)
- Expeditious Synthesis of Isoquinolones and Isocoumarins with a Vinyl Borane as an Acetylene Equivalent. (2016) (17)
- Deciphering isozyme function: exploring cell biology with chemistry in the post-genomic era. (1996) (16)
- Abstract 44: The discovery of ARV-471, an orally bioavailable estrogen receptor degrading PROTAC for the treatment of patients with breast cancer (2021) (16)
- Construction of Highly Substituted Stereodefined Dienes by Cross‐Coupling of α‐Allenic Acetates (2007) (16)
- HIV protease-mediated activation of sterically capped proteasome inhibitors and substrates. (2011) (16)
- Mechanistic basis and efficacy of targeting β-catenin-TCF7L2-JMJD6-MYC axis to overcome resistance to BET inhibitors. (2019) (15)
- Characterization of a novel mammalian phosphatase having sequence similarity to Schizosaccharomyces pombe PHO2 and Saccharomyces cerevisiae PHO13. (2002) (14)
- Identification and Characterization of a Peptidic Ligand for Ras (2010) (14)
- Abstract 43: Discovery of ARV-110, a first in class androgen receptor degrading PROTAC for the treatment of men with metastatic castration resistant prostate cancer (2021) (13)
- Chemical Genetics A Small Molecule Approach to Neurobiology (2002) (13)
- Myriaporone 3/4 structure--activity relationship studies define a pharmacophore targeting eukaryotic protein synthesis. (2006) (12)
- Targeting cyst initiation in ADPKD. (2009) (11)
- BET proteolysis targeted chimera-based therapy of novel models of Richter Transformation-diffuse large B-cell lymphoma (2021) (10)
- Scaffold hopping enables direct access to more potent PROTACs with in vivo activity. (2020) (10)
- Natural Product and Synthetic Proteasome Inhibitors (2004) (10)
- A HaloTag-based small molecule microarray screening methodology with increased sensitivity and multiplex capabilities. (2012) (10)
- Evolving Rules for Protein Degradation? Insights from the Zinc Finger Degrome. (2019) (10)
- Reversal of TNP-470-Induced Endothelial Cell Growth Arrest by Guanine and Guanine Nucleosides (2010) (10)
- Inhibitors of NF-kappaB signaling: design and synthesis of a biotinylated isopanepoxydone affinity reagent. (2002) (9)
- Multiplex CRISPR/Cas screen in regenerating haploid limbs of chimeric Axolotls (2020) (8)
- Hijacking Methyl Reader Proteins for Nuclear-Specific Protein Degradation. (2022) (7)
- BRD4 Proteolysis Targeting Chimera (PROTAC) ARV-825, Causes Sustained Degradation of BRD4 and Modulation of Chemokine Receptors, Cell Adhesion and Metabolic Targets in Leukemia Resulting in Profound Anti-Leukemic Effects (2016) (7)
- Small‐Molecule PROTACS: New Approaches to Protein Degradation (2016) (7)
- The Ubiquitin-Proteasome Pathway and Proteasome Inhibitors (2001) (6)
- Towards the semi-synthesis of didemnin M. Solution and solid phase synthese of the pseudotetrapeptide: pGlu-Glnψ[COO]Ala-Pro-OH (1998) (6)
- Cell Chemical Biology: Home of Exciting Chemical Biology. (2016) (5)
- Using Natural Products to Unravel Cell Biology (2008) (4)
- Generating and identifying axolotls with targeted mutations using Cas9 RNA-guided nuclease. (2015) (4)
- Identification of MAC1: A Small Molecule That Rescues Spindle Bipolarity in Monastrol-Treated Cells. (2016) (4)
- Unexpected stereochemical tolerance for the biological activity of tyroscherin. (2011) (4)
- Chemical Genetics: Exploring the Role of the Proteasome in Cell Biology Using Natural Products and Other Small Molecule Proteasome Inhibitors (2008) (4)
- Protein degraders enter the clinic — a new approach to cancer therapy (2023) (4)
- OligoTRAFTACs: A generalizable method for transcription factor degradation (2021) (4)
- Abstract P4-04-04: Identification and development of oral estrogen receptor PROTAC degraders for breast cancer (2018) (4)
- BRD4 Degradation By Protacs Represents a More Effective Therapeutic Strategy Than BRD4 Inhibitors in DLBCL (2015) (3)
- PROTAC BET degraders are more broadly effective than BET inhibitors (2016) (3)
- Chapter 1. PROTAC-mediated Target Degradation: A Paradigm Changer in Drug Discovery? (2020) (3)
- Electrophilic Screening Platforms for Identifying Novel Covalent Ligands for E3 Ligases. (2021) (3)
- Abstract PR08: ARV-330: An androgen receptor PROTAC degrader for prostate cancer (2015) (3)
- Voices of Chemical Biology: Charting the Next Decade. (2016) (3)
- Abstract 5637: An oral Androgen Receptor PROTAC degrader for prostate cancer (2017) (2)
- A NEW THERAPEUTIC STRATEGY FOR TAUOPATHIES: DISCOVERY OF HIGHLY POTENT BRAIN PENETRANT PROTACTM DEGRADER MOLECULES THAT TARGET PATHOLOGIC TAU PROTEIN SPECIES (2019) (2)
- Regeneration writ large. (2018) (2)
- Regulated Induced Proximity Targeting Chimeras (RIPTACs): a Novel Heterobifunctional Small Molecule Therapeutic Strategy for Killing Cancer Cells Selectively (2023) (2)
- Remembering where we are: Positional information in salamander limb regeneration (2020) (2)
- Author response: Lineage tracing of genome-edited alleles reveals high fidelity axolotl limb regeneration (2017) (2)
- Inhibitors of NF-ϰB Signaling: Design and Synthesis of a Biotinylated Isopanepoxydone Affinity Reagent. (2003) (2)
- Superior Lethal Activity of Novel BET Protein Proteolysis Targeting Chimera (BETP-PROTACs) Versus Betp Bromodomain Inhibitor (BETi) Against Post-Myeloproliferative Neoplasm (MPN) Secondary (s) AML Cells (2016) (1)
- BRD4 degraders produce long-lasting loss of BRD4 Ppotein and robust efficacy in Burkitt’s lymphoma cells. (2015) (1)
- Probing protein function with small molecules. (2006) (1)
- Compounds for enzyme inhibition of proteasome. (2005) (1)
- Raf-1 forms a stable complex with Mekl and activates Mekl by serine phosphorylation ( mitogen-activated protein kinase / protein kinases / signal transduction ) (2005) (1)
- Targeted Dephosphorylation of Tau by Phosphorylation Targeting Chimeras (PhosTACs) as a Therapeutic Modality. (2023) (1)
- Targeted protein degradation: expanding the toolbox (2019) (1)
- Synthesis of Isoquinolones by Sequential Suzuki Coupling of 2-Halobenzonitriles with Vinyl Boronate Followed by Cyclization. (2021) (1)
- Targeted Degradation of mRNA Decapping Enzyme DcpS by a VHL-Recruiting PROTAC. (2022) (1)
- Specific Induction of Golgi Stress by Targeted Protein Destabilization (2015) (1)
- Regeneration writ large (2018) (1)
- Crystal structure of the halotag2 protein at the resolution 2.3A, Northeast Structural Genomics Consortium (NESG) target OR150 (2013) (1)
- Abstract LB-097: Targeted degradation of the androgen receptor in prostate cancer (2015) (1)
- Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance (2018) (1)
- Abstract 5067: BET protein proteolysis targeting chimera (BETP-PROTACs) exert more potent activity than BETP bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm (MPN) secondary (s) AML cells (2017) (1)
- X-Ray Structure of the complex HaloTag2 with HALTS. Northeast Structural Genomics Consortium (NESG) Target OR150. (2013) (0)
- Author response: Multiplex CRISPR/Cas screen in regenerating haploid limbs of chimeric Axolotls (2019) (0)
- Reflecting on the past and looking forward to the future of bridging chemistry and biology. (2014) (0)
- PROTAC-mediated Protein Degradation: A New Therapeutic Modality (2019) (0)
- Faculty Opinions recommendation of A methionine aminopeptidase-2 inhibitor, PPI-2458, for the treatment of rheumatoid arthritis. (2004) (0)
- Compounds for proteasome inhibition of enzymes (2005) (0)
- From Powerful Review Articles to Research Breakthroughs. (2016) (0)
- Composes d'inhibition enzymatique proteasome (2005) (0)
- Life on the edge: Therapeutic uses of cytotoxic natural products (2007) (0)
- Something Old, Something New (2009) (0)
- Reconstitution of the Raf-1-MEK-ERK signal transduction pathway in vitro (1993) (0)
- Development of an Orthogonal tRNA Synthetase for Site-Specific β-Amino Acid Incorporation in Vivo (2017) (0)
- Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase (2019) (0)
- Creation and Characterization of PEG Hydrogels to Observe Neural Stem Cell Chemotaxis (2019) (0)
- Mutations in Yeast Methionine Aminopeptidase-2 Interfere with Binding of the Anti-Angiogenic Agent Fumagillin (2008) (0)
- pVHL54-213-EloB-EloC complex _ methyl 4-(((2S,4R)-4-hydroxy-1-(2-(3- methylisoxazol-5-yl)acetyl)pyrrolidine-2-carboxamido)methyl)benzoate (2012) (0)
- HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH ANGIOGENESIS INHIBITOR FUMAGILLIN (1999) (0)
- Compounds for proteasomenzyminhibering (2005) (0)
- von Hippel-Lindau protein-ElonginB-ElonginC complex, bound to Hif1- alpha peptide (2012) (0)
- Composes d'inhibition enzymatique (2005) (0)
- HUMAN METHIONINE AMINOPEPTIDASE 2 (1999) (0)
- Small molecule‐induced catalytic ubiquitination of non‐natural substrates (2015) (0)
- Construction of Highly Substituted Stereodefined Dienes by Cross‐Coupling of α‐Allenic Acetates. (2007) (0)
- pVHL54-213-EloB-EloC complex (4R)-4-HYDROXY-1-[(3-METHYLISOXAZOL-5-YL)ACETYL]-N-[4-(1,3-OXAZOL-5-YL)BENZYL]-L-PROLINAMIDE bound (2012) (0)
- Efficient Stereoselective Syntheses of Isopanepoxydone and Panepoxydone: A Reassignment of Relative Configuration. (2001) (0)
- Mek: MAPK/Erk kinase (vertebrates) (MAP kinase kinase, MAPKK) (1995) (0)
- Chemistry & Biology editors announce changes to the editorial team. (2011) (0)
- Chemical Genomics: Exploring Biology with Small Organic Molecules (2012) (0)
- Hijacking Methyl Reader Proteins for Nuclear-Specific Protein Degradation (2022) (0)
- Enzymatic compounds for proteasome inhibition (2005) (0)
- An oral androgen receptor RIPTAC for prostate cancer. (2023) (0)
- Abstract 1629: Prostate cancer RIPTAC™ therapeutics demonstrate activity in preclinical models of Enzalutamide-resistant prostate cancer (2023) (0)
- Our Advisors, Our Ambassadors, Our Editorial Board Members. (2016) (0)
- Abstract S4-03: Targeted and selective degradation of estrogen receptor (ER) alpha by PROTACs (2017) (0)
- Expressed in Murine Tissues (1993) (0)
- News from the Chemistry & Biology editorial team. (2012) (0)
- X-Ray Structure of the complex of Haloalkane dehalogenase HaloTag7 with HALTS, Northeast Structural Genomics Consortium (NESG) Target OR151 (2013) (0)
- Chapter 3:Targeted Intracellular Protein Degradation as a Potential Therapeutic Strategy (2010) (0)
- Targeted Therapy for AML Expressing RUNX1 Mutation (2017) (0)
- Generation of Chimeric Axolotls with Mutant Haploid Limbs Through Embryonic Grafting. (2020) (0)
- Total Synthesis of TMC‐95A and ‐B via a New Reaction Leading to Z‐Enamides. Some Preliminary Findings as to SAR. (2004) (0)
- Cutting complexity down to size: Structural and mutational studies of the eukaryotic 20S proteasome (2000) (0)
- Compounds for proteasomenzymhemmung (2005) (0)
- Reconstitution oftheRaf-1-MEK-ERKSignal Transduction PathwayInVitro (1993) (0)
- Composes pour l'inhibition enzymatique (2005) (0)
- Faculty Opinions recommendation of Complementary whole-genome technologies reveal the cellular response to proteasome inhibition by PS-341. (2002) (0)
- Abstract LB-010: Hijacking the E3 ubiquitin ligase cereblon to create efficient BRD4 degraders (2015) (0)
- pVHL-ELOB-ELOC complex_(2S,4R)-1-(3-amino-2-methylbenzoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide bound (2012) (0)
- pVHL:EloB:EloC complex, in complex with capped Hydroxyproline (2012) (0)
- Faculty Opinions recommendation of Identification of genes needed for regeneration, stem cell function, and tissue homeostasis by systematic gene perturbation in planaria. (2005) (0)
- pVHL54-213-EloB-EloC complex _ (2S,4R)-N-((1,1'-biphenyl)-4-ylmethyl)- 4-hydroxy-1-(2-(3-methylisoxazol-5-yl)acetyl)pyrrolidine-2- carboxamide (2012) (0)
- 39 INVITED Targeting steroid hormone receptors for ubiquitination and degradation in breast and prostate cancer (2008) (0)
- Crystal Structure of Haloalkane dehalogenase HaloTag7 at the resolution 1.5A, Northeast Structural Genomics Consortium (NESG) Target OR151 (2013) (0)
- Protechials: A novel approach to pharmacological inhibition of protein function (2001) (0)
- Characterization of a Small‐molecule Modulator of IRE1α Activity (2015) (0)
- pVHL-EloB-EloB-EloC complex_(2S,4R)-1-(2-chlorophenyl)carbonyl-N-[(4-chlorophenyl)methyl]-4-oxidanyl-pyrrolidine-2-carboxamide bound (2012) (0)
- pVHL54-213-EloB-EloC complex_apo (2012) (0)
- Synthesis of 9‐Fluorenylmethoxycarbonyl‐Protected Amino Aldehydes. (1998) (0)
- pVHL54-213-EloB-EloC complex_(2S,4R)-4-hydroxy-1-(2-(3-methylisoxazol- 5-yl)acetyl)-N-(4-nitrobenzyl)pyrrolidine-2-carboxamide bound (2012) (0)
- Retraction of “Targeted Protein Internalization and Degradation by ENDosome TArgeting Chimeras (ENDTACs)” (2020) (0)
- Preclinical Activity of Novel BET Protein Proteolysis Targeting Chimeras (BETP-PROTACs) and Their Combination with Venetoclax or CDK4/6 Inhibitor Against Human Mantle Cell Lymphoma (MCL) Cells (2017) (0)
- Novel BET Protein Proteolysis Targeting Chimeras (BETP-PROTACs) Exert Potent Single Agent and Synergistic Activity with Ibrutinib and Venetoclax Against Human Mantle Cell Lymphoma Cells (2016) (0)
- Life mimics art (2023) (0)
- Towards the Semi‐Synthesis of Didemnin M. Solution and Solid Phase Syntheses of the Pseudotetrapeptide: pGlu‐GlnΨ[COO]Ala‐Pro‐OH. (1998) (0)
- Abstract 4710: BRD4 degradation by PROTACs represents a more effective therapeutic strategy than BRD4 inhibitors in ovarian cancer (2016) (0)
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