Nathanael Gray

Q: What Schools Are Affiliated With Nathanael Gray

Nathanael Gray is affiliated with the following schools: University of California, Berkeley, University of Freiburg, Stanford University, University of North Carolina at Chapel Hill, Harvard University

Nathanael Gray's AcademicInfluence.com Rankings

Nathanael Gray

Medical

#700

World Rank

#928

Historical Rank

Pharmacology

#58

World Rank

#79

Historical Rank

medical Degrees

Nathanael Gray

Chemistry

#888

World Rank

#1451

Historical Rank

Organic Chemistry

#151

World Rank

#192

Historical Rank

chemistry Degrees

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Chemistry

Nathanael Gray's Degrees

PhD Chemistry University of California, Berkeley
Bachelors Chemistry University of California, Berkeley

Why Is Nathanael Gray Influential?

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According to Wikipedia, Nathanael S. Gray is a Krishnan-Shah Family Professor of chemical and systems biology at Stanford University and director of cancer therapeutics programme at Stanford University School of Medicine. Previously he was a Nancy Lurie Marks Professor of biological chemistry and molecular pharmacology at Harvard Medical School and professor of cancer biology at Dana–Farber Cancer Institute. Gray is also co-founder, science advisory board member and equity holder in C4 Therapeutics, Gatekeeper, Syros, Petra, B2S, Aduro, Jengu, Allorion, Inception Therapeutics, and Soltego . C4 Therapeutics, which offered IPO in 2020, was founded based on the ground-breaking research of Jay Bradner, current president of Novartis Institutes for BioMedical Research , and of Nathanael S. Gray, while he was professor at Harvard Medical School. Before moving to Stanford University, Nathanael S. Gray created Center for Protein Degradation at Harvard Medical School with $80 million agreement with Deerfield Management venture capital firm. In 2020, Gray Lab permanently moved to Stanford University, that was stated by Stuart Schreiber, co-founder of Broad Institute as "Stanford's huge gain".

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Nathanael Gray'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

Targeting cancer with small molecule kinase inhibitors (2009) (2351)
Systematic identification of genomic markers of drug sensitivity in cancer cells (2012) (2134)
A Next Generation Connectivity Map: L1000 Platform and the First 1,000,000 Profiles (2017) (1706)
An ATP-competitive Mammalian Target of Rapamycin Inhibitor Reveals Rapamycin-resistant Functions of mTORC1* (2009) (1684)
A unifying model for mTORC1-mediated regulation of mRNA translation (2012) (1260)
A Landscape of Pharmacogenomic Interactions in Cancer (2016) (1254)
DEPTOR Is an mTOR Inhibitor Frequently Overexpressed in Multiple Myeloma Cells and Required for Their Survival (2009) (1163)
A chemical switch for inhibitor-sensitive alleles of any protein kinase (2000) (1035)
The mTOR-Regulated Phosphoproteome Reveals a Mechanism of mTORC1-Mediated Inhibition of Growth Factor Signaling (2011) (1018)
Rational design of inhibitors that bind to inactive kinase conformations (2006) (958)
EML4-ALK Fusion Gene and Efficacy of an ALK Kinase Inhibitor in Lung Cancer (2008) (923)
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M (2009) (886)
Activating mutations in ALK provide a therapeutic target in neuroblastoma (2008) (830)
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. (1998) (761)
Targeting transcription regulation in cancer with a covalent CDK7 inhibitor (2014) (646)
Systematic Identification of Culture Conditions for Induction and Maintenance of Naive Human Pluripotency (2014) (629)
The promise and peril of chemical probes. (2015) (623)
MEK1 mutations confer resistance to MEK and B-RAF inhibition (2009) (616)
Sphingosine 1-Phosphate (S1P) Receptor Subtypes S1P1 and S1P3, Respectively, Regulate Lymphocyte Recirculation and Heart Rate* (2004) (593)
YY1 Is a Structural Regulator of Enhancer-Promoter Loops (2017) (588)
A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. (2011) (578)
Kinase inhibitors: the road ahead (2018) (571)
Developing irreversible inhibitors of the protein kinase cysteinome. (2013) (533)
Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors (2010) (528)
CDK7 Inhibition Suppresses Super-Enhancer-Linked Oncogenic Transcription in MYCN-Driven Cancer (2014) (475)
Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer. (2011) (474)
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen (2008) (423)
Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. (2008) (416)
The dTAG system for immediate and target-specific protein degradation (2018) (415)
mTORC1 Phosphorylation Sites Encode Their Sensitivity to Starvation and Rapamycin (2013) (399)
Activation of tyrosine kinases by mutation of the gatekeeper threonine (2008) (384)
Characterization of a selective inhibitor of the Parkinson’s disease kinase LRRK2 (2011) (383)
CDK4/6 Inhibition Augments Antitumor Immunity by Enhancing T-cell Activation. (2017) (382)
Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor. (2014) (367)
Inhibitor-Sensitive FGFR1 Amplification in Human Non-Small Cell Lung Cancer (2011) (357)
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling (2007) (353)
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK (2007) (348)
Roscovitine Targets, Protein Kinases and Pyridoxal Kinase*[boxs] (2005) (347)
Allosteric inhibitors of Bcr-abl–dependent cell proliferation (2006) (347)
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 (2013) (331)
Factors underlying sensitivity of cancers to small-molecule kinase inhibitors (2009) (328)
Synthetic small molecules that control stem cell fate (2003) (314)
CDK7-Dependent Transcriptional Addiction in Triple-Negative Breast Cancer (2015) (311)
EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors (2015) (307)
Exploration of Type II Binding Mode: A Privileged Approach for Kinase Inhibitor Focused Drug Discovery? (2014) (307)
The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers. (2010) (306)
A PHGDH inhibitor reveals coordination of serine synthesis and 1-carbon unit fate (2016) (306)
A mutation in MYD88 (L265P) supports the survival of lymphoplasmacytic cells by activation of Bruton tyrosine kinase in Waldenström macroglobulinemia. (2013) (299)
Discovery of potent and selective covalent inhibitors of JNK. (2012) (298)
In situ kinase profiling reveals functionally relevant properties of native kinases. (2011) (285)
Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. (2017) (282)
Plasticity in binding confers selectivity in ligand induced protein degradation (2018) (278)
The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma. (2012) (277)
Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor. (2014) (269)
BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment. (2017) (267)
The Library of Integrated Network-Based Cellular Signatures NIH Program: System-Level Cataloging of Human Cells Response to Perturbations. (2017) (267)
Response and acquired resistance to everolimus in anaplastic thyroid cancer. (2014) (264)
Screening of DUB activity and specificity by MALDI-TOF mass spectrometry (2014) (259)
ATP-site directed inhibitors of cyclin-dependent kinases. (1999) (257)
Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors. (2012) (254)
A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader. (2017) (238)
Small molecules that induce cardiomyogenesis in embryonic stem cells. (2004) (231)
Small Molecule Kinase Inhibitors Provide Insight into Mps1 Cell Cycle Function (2010) (226)
Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors. (1999) (225)
Intracellular targets of cyclin-dependent kinase inhibitors: identification by affinity chromatography using immobilised inhibitors. (2000) (225)
Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration (2016) (221)
The Evolving War on Cancer (2011) (218)
A non-canonical SWI/SNF complex is a synthetic lethal target in cancers driven by BAF complex perturbation (2018) (214)
Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors. (2016) (213)
Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. (2010) (209)
Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages (2012) (207)
YAP Drives Growth by Controlling Transcriptional Pause Release from Dynamic Enhancers. (2015) (207)
The Immunological Evolution of Catalysis (1996) (207)
High-throughput kinase profiling as a platform for drug discovery (2008) (205)
The ins and outs of selective kinase inhibitor development. (2015) (202)
Golgicide A reveals essential roles for GBF1 in Golgi assembly and function (2009) (198)
Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. (2010) (195)
The IkappaB Kinase Family Phosphorylates the Parkinson’s Disease Kinase LRRK2 at Ser935 and Ser910 during Toll-Like Receptor Signaling (2012) (195)
Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene. (2010) (193)
A small molecule with osteogenesis-inducing activity in multipotent mesenchymal progenitor cells. (2002) (192)
Small molecule modulators of antioxidant response pathway. (2011) (192)
Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer. (2011) (191)
Structure of the Human cGAS–DNA Complex Reveals Enhanced Control of Immune Surveillance (2018) (187)
Partitioning of cancer therapeutics in nuclear condensates (2020) (187)
Combined EGFR/MEK Inhibition Prevents the Emergence of Resistance in EGFR-Mutant Lung Cancer. (2015) (186)
Treatment-Induced Tumor Dormancy through YAP-Mediated Transcriptional Reprogramming of the Apoptotic Pathway. (2020) (184)
Sphingosine 1-Phosphate ( S 1 P ) Receptor Subtypes S 1 P 1 and S 1 P 3 , Respectively , Regulate Lymphocyte Recirculation and Heart Rate * (2004) (181)
Resistance to irreversible EGF receptor tyrosine kinase inhibitors through a multistep mechanism involving the IGF1R pathway. (2013) (173)
A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics (2014) (171)
In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C (2014) (169)
Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR. (2013) (168)
An efficient rapid system for profiling the cellular activities of molecular libraries. (2006) (168)
Oncogenic PIK3CA-driven mammary tumors frequently recur via PI3K pathway-dependent and -independent mechanisms (2011) (166)
Inhibitor-sensitive FGFR2 and FGFR3 mutations in lung squamous cell carcinoma. (2013) (161)
mTOR Mediated Anti-Cancer Drug Discovery. (2009) (161)
Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. (2012) (158)
Allele-Specific Chromatin Recruitment and Therapeutic Vulnerabilities of ESR1 Activating Mutations. (2018) (158)
Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML. (2019) (155)
A Quantitative Tissue-Specific Landscape of Protein Redox Regulation during Aging (2020) (152)
Acquired resistance of non-small cell lung cancer cells to MET kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency. (2010) (151)
Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands (2018) (148)
A combinatorial scaffold approach toward kinase-directed heterocycle libraries. (2002) (143)
A public-private partnership to unlock the untargeted kinome. (2013) (142)
Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6. (2019) (141)
Pharmacological Targeting of the Pseudokinase Her3 (2014) (141)
CVT-313, a Specific and Potent Inhibitor of CDK2 That Prevents Neointimal Proliferation* (1997) (137)
Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors (2014) (136)
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. (2012) (136)
The LKB1-salt-inducible kinase pathway functions as a key gluconeogenic suppressor in the liver (2014) (135)
A general strategy for creating "inactive-conformation" abl inhibitors. (2006) (135)
Oncogenic PIK 3 CA-driven mammary tumors frequently recur via PI 3 K pathway – dependent and PI 3 K pathway – independent mechanisms (2011) (132)
Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. (2019) (129)
Exploring Targeted Degradation Strategy for Oncogenic KRASG12C. (2019) (128)
CDK12 loss in cancer cells affects DNA damage response genes through premature cleavage and polyadenylation (2018) (127)
A structure-guided approach to creating covalent FGFR inhibitors. (2010) (127)
Small-Molecule Inhibitors of USP1 Target ID1 Degradation in Leukemic Cells (2013) (126)
TYK2-STAT1-BCL2 pathway dependence in T-cell acute lymphoblastic leukemia. (2013) (125)
Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models (2019) (125)
Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. (2013) (124)
Salt-Inducible Kinase 2 Couples Ovarian Cancer Cell Metabolism with Survival at the Adipocyte-Rich Metastatic Niche. (2016) (122)
Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor (2013) (119)
Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development (2020) (119)
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model. (2006) (119)
FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML. (2009) (118)
Progress towards a public chemogenomic set for protein kinases and a call for contributions (2017) (118)
Chaperones as thermodynamic sensors of drug–target interactions reveal kinase inhibitor specificities in living cells (2013) (116)
Synthesis and target identification of hymenialdisine analogs. (2004) (116)
Brain Penetrant LRRK2 Inhibitor. (2012) (115)
SRC family kinases: potential targets for the treatment of human cancer and leukemia. (2003) (113)
Identification of Human Kinases Involved in Hepatitis C Virus Replication by Small Interference RNA Library Screening* (2008) (111)
Metabolic and functional genomic studies identify deoxythymidylate kinase as a target in LKB1-mutant lung cancer. (2013) (111)
Light-induced control of protein destruction by opto-PROTAC (2020) (110)
CDK7 Inhibition Potentiates Genome Instability Triggering Anti-tumor Immunity in Small Cell Lung Cancer. (2019) (109)
A genome-wide overexpression screen in yeast for small-molecule target identification. (2005) (109)
Corrigendum: THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors (2017) (109)
High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors. (2011) (108)
Pharmacological Cyclin-Dependent Kinase Inhibitors Inhibit Replication of Wild-Type and Drug-Resistant Strains of Herpes Simplex Virus and Human Immunodeficiency Virus Type 1 by Targeting Cellular, Not Viral, Proteins (2002) (108)
Inhibiting Fungal Multidrug Resistance by Disrupting an Activator-Mediator Interaction (2016) (107)
Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). (2018) (106)
SIKs control osteocyte responses to parathyroid hormone (2016) (106)
EPHA2 is a mediator of vemurafenib resistance and a novel therapeutic target in melanoma. (2015) (102)
MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells (2014) (102)
Systematic Identification of Culture Conditions for Induction and Maintenance of Naive Human Pluripotency (2014) (102)
A Structure-Based Library Approach to Kinase Inhibitors (1996) (101)
MELK is not necessary for the proliferation of basal-like breast cancer cells (2017) (101)
Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs. (2013) (101)
Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma (2018) (101)
Kinome-wide Selectivity Profiling of ATP-competitive Mammalian Target of Rapamycin (mTOR) Inhibitors and Characterization of Their Binding Kinetics* (2012) (99)
Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C. (2017) (98)
Small-molecule targeting of brachyury transcription factor addiction in chordoma (2019) (98)
Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15 (2019) (94)
EWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma. (2018) (94)
Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC. (2014) (91)
Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations (2019) (90)
Protein kinase IKKβ-catalyzed phosphorylation of IRF5 at Ser462 induces its dimerization and nuclear translocation in myeloid cells (2014) (90)
Repurposing of Kinase Inhibitors for Treatment of COVID-19 (2020) (89)
ALK inhibitor resistance in ALKF1174L-driven neuroblastoma is associated with AXL activation and induction of EMT (2015) (87)
Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13 (2018) (86)
Structural Mechanisms Determining Inhibition of the Collagen Receptor DDR1 by Selective and Multi-Targeted Type II Kinase Inhibitors (2014) (84)
Bruton tyrosine kinase degradation as a therapeutic strategy for cancer. (2019) (83)
SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform. (2018) (82)
Development of Selective Covalent Janus Kinase 3 Inhibitors. (2015) (81)
Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation. (2019) (81)
Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype. (2019) (80)
Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors. (2009) (80)
Molecular rationale for the use of PI3K/AKT/mTOR pathway inhibitors in combination with crizotinib in ALK-mutated neuroblastoma (2014) (80)
Inhibition of USP10 induces degradation of oncogenic FLT3. (2017) (80)
Suppression of Adaptive Responses to Targeted Cancer Therapy by Transcriptional Repression. (2017) (79)
Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules (2020) (78)
EPHA2 Blockade Overcomes Acquired Resistance to EGFR Kinase Inhibitors in Lung Cancer. (2016) (78)
HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib. (2016) (78)
The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma (2014) (77)
Characterization of TAE684 as a potent LRRK2 kinase inhibitor. (2012) (76)
Systematic analysis of BRAFV600E melanomas reveals a role for JNK/c-Jun pathway in adaptive resistance to drug-induced apoptosis (2015) (75)
Pharmacological enhancement of KCC2 gene expression exerts therapeutic effects on human Rett syndrome neurons and Mecp2 mutant mice (2019) (75)
BORIS promotes chromatin regulatory interactions in treatment-resistant cancer cells (2019) (75)
A small-molecule inducer of the antioxidant response element. (2010) (74)
An Embryonic Diapause-like Adaptation with Suppressed Myc Activity Enables Tumor Treatment Persistence. (2021) (74)
Crystal Structure of Pyridoxal Kinase in Complex with Roscovitine and Derivatives* (2005) (74)
Design of allele-specific protein methyltransferase inhibitors. (2001) (72)
Combinatorial synthesis of 2,9-substituted purines (1997) (71)
THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors (2017) (71)
Conformational disturbance in Abl kinase upon mutation and deregulation (2009) (70)
Fibroblast growth factor receptor 1-transformed mammary epithelial cells are dependent on RSK activity for growth and survival. (2009) (70)
Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling (2019) (69)
Activation of HIPK2 Promotes ER Stress-Mediated Neurodegeneration in Amyotrophic Lateral Sclerosis (2016) (68)
Identification of Existing Drugs That Effectively Target NTRK1 and ROS1 Rearrangements in Lung Cancer (2016) (68)
ER Stress Signaling Promotes the Survival of Cancer "Persister Cells" Tolerant to EGFR Tyrosine Kinase Inhibitors. (2018) (66)
Myeloid ERK5 deficiency suppresses tumor growth by blocking protumor macrophage polarization via STAT3 inhibition (2018) (65)
Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors. (2005) (65)
p42/p44 MAPKs are intracellular targets of the CDK inhibitor purvalanol (2002) (64)
Allosteric Interactions between the Myristate- and ATP-Site of the Abl Kinase (2011) (63)
Antimitotic agents of natural origin. (2006) (63)
Selective Mediator-dependence of cell type-specifying transcription (2020) (63)
PIM Kinases Are Essential for Chronic Lymphocytic Leukemia Cell Survival (PIM2/3) and CXCR4-Mediated Microenvironmental Interactions (PIM1) (2014) (63)
Discovery of a Potent, Covalent BTK Inhibitor for B-Cell Lymphoma (2014) (62)
Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases (2013) (61)
A cyclin-dependent kinase inhibitor inducing cancer cell differentiation: biochemical identification using Xenopus egg extracts. (1999) (61)
Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants. (2010) (61)
c-Jun N-terminal kinase promotes stem cell phenotype in triple-negative breast cancer through upregulation of Notch1 via activation of c-Jun (2017) (60)
Discovery of Type II Inhibitors of TGFβ-Activated Kinase 1 (TAK1) and Mitogen-Activated Protein Kinase Kinase Kinase Kinase 2 (MAP4K2) (2014) (60)
A brain-penetrant RAF dimer antagonist for the noncanonical BRAF oncoprotein of pediatric low-grade astrocytomas (2017) (60)
The mechanism of activation of IRAK1 and IRAK4 by interleukin-1 and Toll-like receptor agonists (2017) (60)
Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1 (2011) (60)
Small-molecule screening identifies inhibition of salt-inducible kinases as a therapeutic strategy to enhance immunoregulatory functions of dendritic cells (2014) (60)
Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2 (2020) (60)
Discovery of selective irreversible inhibitors for EGFR-T790M. (2011) (59)
Identification of a novel protein regulating microtubule stability through a chemical approach. (2004) (59)
Discovery of a selective inhibitor of Doublecortin Like Kinase 1 (2020) (59)
Systematic Kinome shRNA Screening Identifies CDK11 (PITSLRE) Kinase Expression Is Critical for Osteosarcoma Cell Growth and Proliferation (2012) (58)
Acquired Resistance to Dasatinib in Lung Cancer Cell Lines Conferred by DDR2 Gatekeeper Mutation and NF1 Loss (2013) (58)
Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8. (2018) (58)
A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl. (2010) (58)
Systematic Identification of Culture Conditions for Induction and Maintenance of Naive Human Pluripotency (2014) (57)
The mitogen-activated protein kinase ERK5 regulates the development and growth of hepatocellular carcinoma (2014) (57)
Enhancer profiling identifies critical cancer genes and characterizes cell identity in adult T-cell leukemia. (2017) (57)
Mitotic MELK-eIF4B signaling controls protein synthesis and tumor cell survival (2016) (57)
Ligand associated ERBB2/3 activation confers acquired resistance to FGFR inhibition in FGFR3 dependent cancer cells (2014) (57)
Activation of the p53 Transcriptional Program Sensitizes Cancer Cells to Cdk7 Inhibitors. (2017) (57)
The PP2A-Integrator-CDK9 axis fine-tunes transcription and can be targeted therapeutically in cancer (2021) (56)
Targeting Pin1 renders pancreatic cancer eradicable by synergizing with immunochemotherapy (2021) (56)
Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site. (2010) (55)
A UV-Independent Topical Small-Molecule Approach for Melanin Production in Human Skin (2017) (55)
Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1. (2006) (55)
Structure-activity relationships and inhibitory effects of various purine derivatives on the in vitro growth of Plasmodium falciparum. (2001) (55)
Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors. (2017) (55)
Development and Characterization of a Wee1 Kinase Degrader. (2019) (54)
BTKCys481Ser drives ibrutinib resistance via ERK1/2 and protects BTKwild-type MYD88-mutated cells by a paracrine mechanism. (2018) (54)
Covalent Guanosine Mimetic Inhibitors of G12C KRAS. (2017) (54)
N-Myristoylated c-Abl Tyrosine Kinase Localizes to the Endoplasmic Reticulum upon Binding to an Allosteric Inhibitor* (2009) (54)
Discovery of estrogen sulfotransferase inhibitors from a purine library screen. (2001) (54)
Inhibition of Flaviviruses by Targeting a Conserved Pocket on the Viral Envelope Protein. (2018) (54)
Mutations in the DDR 2 Kinase Gene identify a Novel therapeutic target in squamous cell lung cancer (2011) (53)
TSC1 involvement in bladder cancer: diverse effects and therapeutic implications (2013) (53)
A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. (2018) (52)
A High-Throughput Immune-Oncology Screen Identifies EGFR Inhibitors as Potent Enhancers of Antigen-Specific Cytotoxic T-lymphocyte Tumor Cell Killing (2018) (51)
Purine‐Based Inhibitors of Inositol‐1,4,5‐trisphosphate‐3‐kinase (2002) (51)
Tivantinib (ARQ 197) efficacy is independent of MET inhibition in non‐small‐cell lung cancer cell lines (2015) (50)
Expanding the Diversity of Allosteric Bcr-Abl Inhibitors† (2010) (50)
Crystal structure of human IRAK1 (2017) (49)
Discovery of Carbohydrate Sulfotransferase Inhibitors from a Kinase‐Directed Library (2000) (49)
GNF-2 Inhibits Dengue Virus by Targeting Abl Kinases and the Viral E Protein. (2016) (48)
Expanding the diversity of purine libraries (2001) (48)
Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo. (2016) (47)
Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. (2006) (47)
A ceramide‐1‐phosphate analogue, PCERA‐1, simultaneously suppresses tumour necrosis factor‐α and induces interleukin‐10 production in activated macrophages (2009) (46)
ULK1 inhibition overcomes compromised antigen presentation and restores antitumor immunity in LKB1 mutant lung cancer (2021) (45)
Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 – 2011) (2012) (45)
Covalent Targeting of Fibroblast Growth Factor Receptor Inhibits Metastatic Breast Cancer (2016) (44)
Development of small molecules targeting the pseudokinase Her3. (2015) (44)
Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations. (2020) (44)
BCL2 Amplicon Loss and Transcriptional Remodeling Drives ABT-199 Resistance in B Cell Lymphoma Models. (2019) (44)
Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo (2021) (44)
Inhibiting the oncogenic translation program is an effective therapeutic strategy in multiple myeloma (2017) (43)
Cheminformatics Tools for Analyzing and Designing Optimized Small-Molecule Collections and Libraries. (2019) (42)
Discovery and resistance mechanism of a selective CDK12 degrader (2021) (42)
Selective Akt Inhibitors Synergize with Tyrosine Kinase Inhibitors and Effectively Override Stroma-Associated Cytoprotection of Mutant FLT3-Positive AML Cells (2013) (42)
The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification (2019) (42)
ERK5 is activated by oncogenic BRAF and promotes melanoma growth (2018) (42)
Development of ATP-competitive mTOR inhibitors. (2012) (42)
DFG-out Mode of Inhibition by an Irreversible Type-1 Inhibitor Capable of Overcoming Gate-Keeper Mutations in FGF Receptors (2014) (41)
Synthetic Lethal Interaction of SHOC2 Depletion with MEK Inhibition in RAS-Driven Cancers. (2019) (41)
High MITF Expression Is Associated with Super-Enhancers and Suppressed by CDK7 Inhibition in Melanoma. (2018) (41)
Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells. (2017) (41)
CDK13 cooperates with CDK12 to control global RNA polymerase II processivity (2020) (40)
Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors. (2001) (40)
Tuning microtubule dynamics to enhance cancer therapy by modulating FER-mediated CRMP2 phosphorylation (2018) (39)
Vomocytosis of live pathogens from macrophages is regulated by the atypical MAP kinase ERK5 (2017) (39)
Specific covalent inhibition of MALT1 paracaspase suppresses B cell lymphoma growth (2018) (39)
Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor. (2015) (39)
Discovery of a selective irreversible BMX inhibitor for prostate cancer. (2013) (38)
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. (2008) (38)
RAS–MAPK Reactivation Facilitates Acquired Resistance in FGFR1-Amplified Lung Cancer and Underlies a Rationale for Upfront FGFR–MEK Blockade (2018) (38)
Dual blockade of lipid and cyclin-dependent kinases induces synthetic lethality in malignant glioma (2012) (38)
Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer (2015) (37)
Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-benzodiazipinones as Inhibitors of Kinases and Bromodomains. (2018) (37)
Discovery of selective aminothiazole aurora kinase inhibitors. (2008) (37)
Chemical and biological profile of dual Cdk1 and Cdk2 inhibitors. (2003) (37)
Discovery of a BTK/MNK dual inhibitor for lymphoma and leukemia (2016) (36)
Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation (2016) (36)
A concise and traceless linker strategy toward combinatorial libraries of 2,6,9-substituted purines. (2001) (36)
Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones (2013) (36)
BMK1 is involved in the regulation of p53 through disrupting the PML-MDM2 interaction (2012) (36)
STRIPAK directs PP2A activity toward MAP4K4 to promote oncogenic transformation of human cells (2020) (35)
Small-molecule inhibitors of the c-Fes protein-tyrosine kinase. (2012) (35)
Erk5 Is a Key Regulator of Naive-Primed Transition and Embryonic Stem Cell Identity (2016) (35)
Interleukin-6 Secretion by Astrocytes Is Dynamically Regulated by PI3K-mTOR-Calcium Signaling (2014) (34)
Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. (2015) (33)
Identification of a potent and selective covalent Pin1 inhibitor (2020) (33)
Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis. (2016) (33)
Resin-capture and release strategy toward combinatorial libraries of 2,6,9-substituted purines. (2002) (32)
Identification of Homeodomain Proteins, PBX1 and PREP1, Involved in the Transcription of Murine Leukemia Virus (2003) (32)
X-ray Crystal Structure of ERK5 (MAPK7) in Complex with a Specific Inhibitor (2013) (32)
Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells (2015) (32)
Defining and Targeting Adaptations to Oncogenic KRASG12C Inhibition Using Quantitative Temporal Proteomics. (2020) (32)
Inhibition of CDK4/6 promotes CD8 T-cell memory formation. (2021) (32)
Digital pattern recognition-based image analysis quantifies immune infiltrates in distinct tissue regions of colorectal cancer and identifies a metastatic phenotype (2013) (32)
Verification of a designed intramolecular hydrogen bond in a drug scaffold by nuclear magnetic resonance spectroscopy. (2007) (32)
Salt-Inducible Kinase inhibition suppresses acute myeloid leukemia progression in vivo. (2019) (31)
Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors. (2019) (31)
Solid-phase synthesis of 2,3,5-trisubstituted indoles. (2001) (31)
Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome. (2019) (31)
Insulin-like growth factor 1 and growth hormone binding protein in depression: a preliminary communication. (1999) (31)
Development of CDK2 and CDK5 Dual Degrader TMX-2172. (2020) (30)
A general strategy for creating (2006) (30)
Pharmacological perturbation of CDK 9 using selective CDK 9 inhibition or degradation (2018) (30)
Fragment-based covalent ligand discovery (2021) (30)
Microenvironmental Influence on Pre-Clinical Activity of Polo-Like Kinase Inhibition in Multiple Myeloma: Implications for Clinical Translation (2011) (30)
Targeting transcription cycles in cancer (2021) (29)
Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma (2020) (29)
Modulation of TNFalpha, IL-10 and IL-12p40 levels by a ceramide-1-phosphate analog, PCERA-1, in vivo and ex vivo in primary macrophages. (2009) (29)
Mammalian cell proliferation requires noncatalytic functions of O-GlcNAc transferase (2020) (28)
Discoidin domain receptor 2 mediates collagen-induced activation of membrane-type 1 matrix metalloproteinase in human fibroblasts (2017) (28)
Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo. (2018) (28)
Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors (2011) (28)
Extracellular signal–regulated kinase 5 promotes acute cellular and systemic inflammation (2015) (28)
Drug discovery through industry-academic partnerships (2006) (27)
A kinase-independent role for CDK8 in BCR-ABL1+ leukemia (2019) (27)
TRIM8 modulates the EWS/FLI oncoprotein to promote survival in Ewing sarcoma (2021) (26)
Inhibitor-Sensitive FGFR 1 Amplification in Human Non-Small Cell Lung Cancer (2011) (26)
Chemical Interrogation of the Malaria Kinome (2014) (26)
Discovery of a potent dual ALK and EGFR T790M inhibitor. (2017) (26)
Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins. (2021) (25)
KRAS G12C Drug Development: Discrimination between Switch II Pocket Configurations Using Hydrogen/Deuterium-Exchange Mass Spectrometry. (2017) (25)
Small-Molecule Inhibitors of LRRK2. (2017) (25)
Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors. (2020) (25)
INK4 Tumor Suppressor Proteins Mediate Resistance to CDK4/6 Kinase Inhibitors (2021) (24)
Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library. (2020) (24)
Leveraging kinase inhibitors to develop small molecule tools for imaging kinases by fluorescence microscopy. (2012) (24)
Leveraging Gas-Phase Fragmentation Pathways for Improved Identification and Selective Detection of Targets Modified by Covalent Probes. (2016) (24)
Identification of novel therapeutic targets in acute leukemias with NRAS mutations using a pharmacologic approach. (2015) (24)
Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I. (2008) (24)
Comparison of effects of midostaurin, crenolanib, quizartinib, gilteritinib, sorafenib and BLU‐285 on oncogenic mutants of KIT, CBL and FLT3 in haematological malignancies (2019) (24)
Prospects for Antibacterial Discovery and Development. (2021) (23)
SYK is activated by mutated MYD88 and drives pro-survival signaling in MYD88 driven B-cell lymphomas (2020) (23)
Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. (2019) (22)
Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials. (2010) (22)
Gemcitabine and Chk1 Inhibitor AZD7762 Synergistically Suppress the Growth of Lkb1-Deficient Lung Adenocarcinoma. (2017) (22)
NVP‐TAE684 reverses multidrug resistance (MDR) in human osteosarcoma by inhibiting P‐glycoprotein (PGP1) function (2016) (22)
Sustained Akt Activity Is Required to Maintain Cell Viability in Seborrheic Keratosis, a Benign Epithelial Tumor. (2016) (22)
GSK 2578215 A ; A potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK 2 kinase inhibitor (2014) (22)
When Kinases Meet PROTACs (2018) (22)
Pharmacological inhibition of Eph receptors enhances glucose-stimulated insulin secretion from mouse and human pancreatic islets (2013) (22)
Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2. (2006) (21)
Corrigendum: A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. (2016) (21)
CDK13 cooperates with CDK12 to control global RNA polymerase II processivity (2020) (21)
Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen. (2012) (21)
Acute pharmacological degradation of Helios destabilizes regulatory T cells (2021) (21)
Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor. (2018) (21)
Structure-guided development of covalent TAK1 inhibitors. (2017) (21)
A-770041 reverses paclitaxel and doxorubicin resistance in osteosarcoma cells (2014) (21)
Combinatorial libraries and biological discovery (2001) (20)
Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors. (2018) (20)
Increased lysosomal biomass is responsible for the resistance of triple-negative breast cancers to CDK4/6 inhibition (2020) (20)
Small Molecules Targeting the Flavivirus E Protein with Broad-Spectrum Activity and Antiviral Efficacy in Vivo. (2019) (20)
Progress on Covalent Inhibition of KRAS(G12C). (2016) (20)
Synergistic interactions with PI3K inhibition that induce apoptosis (2017) (20)
Salt-inducible kinase 1 maintains HDAC7 stability to promote pathologic cardiac remodeling. (2020) (20)
An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer (2022) (20)
Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors (2020) (20)
Chemical proteomics identifies unanticipated targets of clinical kinase inhibitors. (2007) (19)
Discovery of allosteric BCR-ABL inhibitors from phenotypic screen to clinical candidate. (2014) (19)
Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase (2015) (19)
Targeting the Extracellular Signal-Regulated Kinase 5 Pathway to Suppress Human Chronic Myeloid Leukemia Stem Cells (2018) (19)
Broad spectrum alkynyl inhibitors of T315I Bcr-Abl. (2010) (19)
Discovery and Characterization of Novel Mutant FLT3 Kinase Inhibitors (2010) (18)
Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model (2017) (18)
Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13. (2020) (18)
Increased lysosomal biomass is responsible for the resistance of triple-negative breast cancers to CDK4/6 inhibition. (2020) (17)
Discovery of Covalent CDK14 Inhibitors with Pan-TAIRE Family Specificity. (2019) (17)
Cell-based optimization of novel benzamides as potential antimalarial leads (2009) (16)
SnapShot: Kinase Inhibitors I. (2015) (16)
Discovery of Immunologically Inspired Small Molecules That Target the Viral Envelope Protein. (2018) (16)
Discovery of 1-( 4-( 4-Propionylpiperazin-1-yl )-3-( trifluoromethyl ) phenyl )-9-( quinolin-3-yl ) benzo [ h ] [ 1 , 6 ] naphthyridin-2 ( 1 H )-one as a Highly Potent (2014) (16)
Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor. (2016) (16)
Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma. (2021) (16)
Inhibition of the deubiquitinase USP10 induces degradation of SYK (2020) (16)
Fluorescent Visualization of Src by Using Dasatinib‐BODIPY (2014) (16)
Fibroblast growth factor receptor 1-transformed mammary epithelial cells are dependent on RSK activity for growth and survival (Cancer Research (2009) 69 (2244-2251)) (2009) (16)
Chemical Biology Toolkit for DCLK1 Reveals Connection to RNA Processing. (2020) (16)
Selective ATP-competitive inhibitors of TOR suppress rapamycin-insensitive function of TORC2 in Saccharomyces cerevisiae. (2012) (16)
Upregulation of IGF1R by Mutant RAS in Leukemia and Potentiation of RAS Signaling Inhibitors by Small-Molecule Inhibition of IGF1R (2014) (16)
Suppression of interferon β gene transcription by inhibitors of bromodomain and extra-terminal (BET) family members (2015) (15)
First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia. (2018) (15)
Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors. (2017) (15)
Discovery of host‐targeted covalent inhibitors of dengue virus (2017) (14)
How small-molecule inhibitors of dengue-virus infection interfere with viral membrane fusion (2018) (14)
TYK 2 – STAT 1 – BCL 2 Pathway Dependence in T-cell Acute Lymphoblastic Leukemia (2013) (14)
Peptide-based covalent inhibitors of MALT1 paracaspase. (2019) (14)
Identification and characterization of small-molecule inducers of epidermal keratinocyte differentiation. (2007) (14)
Pathophysiological significance and therapeutic targeting of germinal center kinase in diffuse large B-cell lymphoma. (2016) (14)
PI3K/AKT Pathway Is Activated By MYD88 L265P and Use Of PI3K-Delta Inhibitors Induces Robust Tumor Cell Killing In Waldenstrom’s Macroglobulinemia (2013) (14)
Discovery of a Highly Selective STK16 Kinase Inhibitor. (2016) (14)
Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors. (2017) (14)
BAY61-3606 Affects the Viability of Colon Cancer Cells in a Genotype-Directed Manner (2012) (14)
Dual inhibition of Fes and Flt3 tyrosine kinases potently inhibits Flt3-ITD+ AML cell growth (2017) (13)
Synthesis and structure activity relationships of DCLK1 kinase inhibitors based on a 5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one scaffold. (2020) (13)
Structure-based design of a potent and selective covalent inhibitor for SRC kinase that targets a p-Loop cysteine. (2020) (13)
BMX-Mediated Regulation of Multiple Tyrosine Kinases Contributes to Castration Resistance in Prostate Cancer. (2018) (13)
Catalytic domain plasticity of MKK7 reveals structural mechanisms of allosteric activation and new targeting opportunities (2020) (13)
Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent. (2017) (13)
JNK2 Is Required for the Tumorigenic Properties of Melanoma Cells. (2019) (13)
in squamous cell lung cancer (2011) (13)
Effects of the multi‐kinase inhibitor midostaurin in combination with chemotherapy in models of acute myeloid leukaemia (2020) (13)
Targeting oncoproteins with a positive selection assay for protein degraders (2020) (13)
Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2. (2021) (13)
Inhibition of IKKα by BAY61-3606 Reveals IKKα-Dependent Histone H3 Phosphorylation in Human Cytomegalovirus Infected Cells (2016) (13)
A benzo[b]thiophene-based selective type 4 S1P receptor agonist. (2017) (13)
Extracellular-Regulated Protein Kinase 5-Mediated Control of p21 Expression Promotes Macrophage Proliferation Associated with Tumor Growth and Metastasis (2020) (13)
PRM-LIVE with Trapped Ion Mobility Spectrometry and Its Application in Selectivity Profiling of Kinase Inhibitors. (2021) (13)
Targeting IRAK1/IRAK4 Signaling in Waldenstrom's Macroglobulinemia (2015) (13)
Discovery and Structure-Activity Relationship Study of (Z)-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors. (2020) (13)
Targeting Myddosome Assembly in Waldenstrom Macroglobulinaemia (2017) (13)
Discovery of a Potent and Selective DDR 1 Receptor Tyrosine Kinase Inhibitor (2013) (12)
The HCK/BTK inhibitor KIN-8194 is active in MYD88 driven lymphomas and overcomes mutated BTKCys481 ibrutinib resistance. (2021) (12)
Inhibitor-Sensitive FGFR 2 and FGFR 3 Mutations in Lung Squamous Cell Carcinoma (2013) (12)
Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface. (2020) (12)
Tubulin Resists Degradation by Cereblon-Recruiting PROTACs (2020) (12)
Discovery of a Series of 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-ones as Selective PI3K-δ/γ Inhibitors. (2016) (12)
Identification of small molecule inhibitors targeting the Zika virus envelope protein. (2019) (11)
Development of 'DFG-out' inhibitors of gatekeeper mutant kinases. (2012) (11)
Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors. (2020) (11)
An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFRα and kit. (2012) (11)
Abstract 2: FGFR3 as a therapeutic target in squamous cell lung carcinoma (2012) (10)
Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold. (2019) (10)
Torin2 Suppresses Ionizing Radiation-Induced DNA Damage Repair (2016) (10)
Targeted brachyury degradation disrupts a highly specific autoregulatory program controlling chordoma cell identity (2021) (10)
Characterization of a highly selective inhibitor of the Aurora kinases. (2017) (10)
Structure and Characterization of a Covalent Inhibitor of Src Kinase (2020) (10)
Genomic and pathological heterogeneity in clinically diagnosed small cell lung cancer in never/light smokers identifies therapeutically targetable alterations (2020) (10)
Identification of compounds with anti-human cytomegalovirus activity that inhibit production of IE2 proteins (2017) (10)
A Discovery Strategy for Selective Inhibitors of c‐Src in Complex with the Focal Adhesion Kinase SH3/SH2‐binding Region (2015) (10)
SnapShot: Kinase Inhibitors II. (2015) (10)
Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability. (2011) (10)
Exploring the target scope of KEAP1 E3 ligase-based PROTACs. (2022) (9)
A multitargeted probe-based strategy to identify signaling vulnerabilities in cancers (2019) (9)
What It Takes to Improve a First-Generation Inhibitor to a Second- or Third-Generation Small Molecule. (2019) (9)
Correction: MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells (2014) (9)
Sulfopin, a selective covalent inhibitor of Pin1, blocks Myc-driven tumor initiation and growth in vivo (2020) (9)
Coordinating Tissue Regeneration Through Transforming Growth Factor‐β Activated Kinase 1 Inactivation and Reactivation (2019) (9)
Quinoline and thiazolopyridine allosteric inhibitors of MALT1. (2019) (9)
A novel HER2-selective kinase inhibitor is effective in HER2 mutant and amplified non-small cell lung cancer. (2022) (9)
Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors (2022) (9)
Purine-Based Inhibitors of Inositol1,4,5-trisphosphate-3-kinase (2010) (8)
Evaluation of ERK as a therapeutic target in acute myelogenous leukemia (2019) (8)
Immune response to COVID‐19 vaccination is attenuated by poor disease control and antimyeloma therapy with vaccine driven divergent T‐cell response (2021) (8)
Resistance to Irreversible EGFR Tyrosine Kinase Inhibitors through a Multistep Mechanism Involving the IGF 1 R Pathway (2012) (8)
Cancer stem cell marker DCLK1 reprograms small extracellular vesicles toward migratory phenotype in gastric cancer cells (2021) (8)
Systematic analysis of BRAFV 600 E melanomas reveals a role for JNK / c-Jun pathway in adaptive resistance to drug-induced apoptosis (2015) (7)
The Dawn of Allosteric BCR-ABL1 Drugs: From a Phenotypic Screening Hit to an Approved Drug. (2022) (7)
Discovery of 9-(6-aminopyridin-3-yl)-1-(3- (trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective and orally available mTOR inhibitor for treatment of cancer (2011) (7)
1,4,5-trisphosphate-3-kinase (2002) (7)
Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216. (2021) (7)
Synergistic Anti-Tumor Effect of Combining Selective CDK7 and BRD4 Inhibition in Neuroblastoma (2022) (7)
HCK Is a Highly Relevant Target of Ibrutinib in MYD88 Mutated Waldenstrom's Macroglobulinemia and Diffuse Large B-Cell Lymphoma (2015) (7)
Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor–associated kinase 4 (IRAK4) (2019) (7)
Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma. (2020) (7)
Discovery and Optimization of Tau Targeted Protein Degraders Enabled by Patient Induced Pluripotent Stem Cells-Derived Neuronal Models of Tauopathy (2022) (7)
Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II. (2009) (6)
Benzopyrimidodiazepinone inhibitors of TNK2. (2020) (6)
Current Therapies Under Investigation for COVID-19. (2020) (6)
Discovery of Covalent MKK4/7 Dual Inhibitor. (2020) (6)
Publication Criteria and Requirements for Studies on Protein Kinase Inhibitors─What Is Expected? (2022) (6)
A Novel, Highly Selective IRAK1 Inhibitor Jh-X-119-01 Shows Synergistic Tumor Cell Killing with Ibrutinib in MYD88 Mutated B-Cell Lymphoma Cells (2017) (6)
Anti‐SARS‐CoV‐2 activity of targeted kinase inhibitors: Repurposing clinically available drugs for COVID‐19 therapy (2022) (6)
Cheminformatics Tools for Analyzing and Designing Optimized Small Molecule Collections and Libraries (2018) (6)
Selective degradation-inducing probes for studying cereblon (CRBN) biology. (2021) (5)
Dual targeting of salt inducible kinases and CSF1R uncouples bone formation and bone resorption (2021) (5)
Defining and targeting adaptations to oncogenic KRASG12C inhibition using quantitative temporal proteomics (2019) (5)
Expanding the Diversity of Purine Libraries. (2002) (5)
Protected Amine Labels: A Versatile Molecular Scaffold for Multiplexed Nominal Mass and Sub-Da Isotopologue Quantitative Proteomic Reagents (2014) (5)
Corrigendum: The promise and peril of chemical probes. (2015) (5)
Small Molecule Inhibitors of ALK (2017) (4)
A Novel HCK and BTK Dual Inhibitor Kin-8194 Shows Superior Activity over Ibrutinib and Overcomes BTKC481S Mediated Ibrutinib Resistance in Vitro and In Vivo in MYD88 Mutated B-Cell Lymphomas (2019) (4)
Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor. (2020) (4)
Cheminformatics tools for analyzing and designing optimized small molecule libraries (2018) (4)
Erratum: The promise and peril of chemical probes (Nature Chemical Biology (2015) 11 (536-541)) (2015) (4)
Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation (2021) (4)
BTK drives ibrutinib resistance via ERK1/2, and protects BTK MYD88 mutated cells by a paracrine mechanism (2018) (4)
Corrigendum: SIKs control osteocyte responses to parathyroid hormone (2017) (4)
Abstract 4832: Novel EGFR mutations that cause drug resistance to irreversible pyrimidine but not quinazoline based EGFR inhibitors (2012) (4)
Abstract 4935: High-throughput immune-oncology screen identifies EGFR inhibitors as potent enhancers of CTL antigen-specific tumor cell killing (2018) (4)
Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14. (2019) (3)
Acute pharmacological degradation of ERK5 does not inhibit cellular immune response or proliferation. (2022) (3)
Kang Starvation and Rapamycin mTORC 1 Phosphorylation Sites Encode Their Sensitivity to (2013) (3)
University of Dundee The LKB 1-salt-inducible kinase pathway functions as a key gluconeogenic suppressor in the liver (2014) (3)
A broad-spectrum antiviral molecule, QL47, selectively inhibits eukaryotic translation (2019) (3)
Development of Highly Potent and Selective Pyrazolopyridine Inhibitor of CDK8/19. (2021) (3)
Dissection of Bcr-abl Structural Domains Relating to Kinase Auto-Inhibition Using a Forward Mutational Screen with the Non-ATP Competitive Inhibitor GNF-2. (2007) (3)
A Simple Method to Identify Kinases That Regulate Embryonic Stem Cell Pluripotency by High-throughput Inhibitor Screening (2017) (3)
A PP2A-Integrator complex fine-tunes transcription by opposing CDK9 (2020) (3)
Discovery of Novel 1H‐Imidazol‐2‐yl‐pyrimidine‐4,6‐diamines as Potential Antimalarials. (2010) (3)
Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC. (2022) (3)
Unleashing Cell-Intrinsic Inflammation As a Strategy to Kill AML Blasts (2021) (3)
Chemically Induced Degradation of MALT1 to Treat B-Cell Lymphomas (2019) (3)
Temporal resolution of gene derepression and proteome changes upon PROTAC-mediated degradation of BCL11A protein in erythroid cells. (2022) (3)
Generation of a chemical genetic model for JAK3 (2021) (3)
Correction to Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor (2014) (3)
A preclinical platform for assessing antitumor effects and systemic toxicities of cancer drug targets (2022) (3)
Discovery of a Series of Benzopyrimidodiazepinone TNK2 Inhibitors via Scaffold Morphing. (2020) (3)
Characterization of Torin 2 , an ATP-Competitive Inhibitor of mTOR , ATM , and ATR Citation (2013) (2)
Abstract B165: Optimizing selective CDK7 inhibition in MYCN-driven neuroblastoma (2015) (2)
Novel Macrocyclic Peptidomimetics Targeting the Polo-Box Domain of Polo-Like Kinase 1. (2022) (2)
Targeting the PI5P4K lipid kinase family in cancer using novel covalent inhibitors (2019) (2)
Targeting EGFR in glioblastoma with a novel brain-penetrant small molecule EGFR-TKI (2021) (2)
Synthesis and structure-activity relationships of targeted protein degraders for the understudied kinase NEK9 (2021) (2)
The Cyclin-Dependent Kinase 8 (CDK8) Inhibitor DCA Promotes a Tolerogenic Chemical Immunophenotype in CD4+ T Cells via a Novel CDK8-GATA3-FOXP3 Pathway (2021) (2)
Erratum: Targeting Transcriptional Addictions in Small Cell Lung Cancer with a Covalent CDK7 Inhibitor (Cancer Cell (2014) 26(6) (909–922) (S1535610814004231) (10.1016/j.ccell.2014.10.019)) (2015) (2)
A Community of Agents Maintaining Link Integrity in the World Wide Web (1998) (2)
Inhibiting ERK5 Overcomes Breast Cancer Resistance to Anti-HER2 Therapy By Targeting the G1–S Cell-Cycle Transition (2022) (2)
CM93, a novel covalent small molecule inhibitor targeting lung cancer with mutant EGFR (2020) (2)
Cereblon covalent modulation through structure-based design of histidine targeting chemical probes (2022) (2)
Retraction Notice to: Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2 (2022) (2)
Cancer Biology and Signal Transduction Acquired Resistance to Dasatinib in Lung Cancer Cell Lines Conferred by DDR 2 Gatekeeper Mutation and NF 1 Loss (2014) (2)
Exploring Ligand-Directed N-Acyl-N-alkylsulfonamide-Based Acylation Chemistry for Potential Targeted Degrader Development. (2021) (2)
Systematic Characterization of Genes Representing Preferential Molecular Vulnerabilities for Myeloma Cells Compared to Other Neoplasias - Implications for the Biology and Therapeutic Targeting of Myeloma (2019) (2)
The ETS transcription factor ETV6 constrains the transcriptional activity of EWS–FLI to promote Ewing sarcoma (2023) (2)
Correction: An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. (2020) (2)
A broad-spectrum antiviral molecule, QL47, selectively inhibits eukaryotic translation. (2020) (2)
Chemical and Biological Profile of Dual Cdk 1 and Cdk 2 Inhibitors (2011) (2)
Synthesis and Structure-Activity relationships of cyclin-dependent kinase 11 inhibitors based on a diaminothiazole scaffold. (2022) (2)
Therapeutics , Targets , and Chemical Biology Resistance to Irreversible EGF Receptor Tyrosine Kinase Inhibitors through a Multistep Mechanism Involving the IGF 1 R Pathway (2013) (2)
Author response: MELK is not necessary for the proliferation of basal-like breast cancer cells (2017) (2)
It Takes Two To Target: A Study in KRAS Dimerization. (2018) (2)
297 Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC (2014) (1)
Inhibition of USP10 Induces Degradation of Oncogenic FLT3: A Novel Approach to Therapy of Leukemia (2016) (1)
Selective ATP-Competitive Inhibitors of TOR Suppress Rapamycin-Insensitive Function of TORC2 in S. cerevisiae (2012) (1)
Abstract 4736: Amplification of ERK2 mediates resistance to the novel irreversible EGFR inhibitor WZ4002 (2011) (1)
A Novel HCK Inhibitor Kin-8193 Blocks BTK Activity in BTKCys481 Mutated Ibrutinib Resistant B-Cell Lymphomas Driven By Mutated MYD88 (2018) (1)
Abstract A234: Identification and characterization of inhibitor-resistant mutants of the protein-tyrosine kinase c-Fes. (2011) (1)
Development and utility of a PAK1-selective degrader (2022) (1)
Selectivity and binding kinetics of mTOR inhibitors 1 Kinome-wide selectivity profiling of ATP-competitive mTOR ( mammalian target of rapamycin ) inhibitors and characterization of their binding kinetics (2011) (1)
MALT1 Degradation with a Proteolysis-Targeting Chimera for the Treatment of Activated B-Cell Type Diffuse Large B-Cell Lymphoma (2021) (1)
The kinase activity of the cancer stem cell marker DCLK1 drives gastric cancer progression by reprogramming the stromal tumor landscape (2022) (1)
Serine/Threonine Kinase STK4 Is a Novel Target in Myeloma (2014) (1)
Allele-Specific Chromatin Recruitment and Therapeutic Vulnerabilities of ESR 1 Activating Mutations Graphical Abstract Highlights (2018) (1)
Covalent disruptor of YAP-TEAD association suppresses defective Hippo signaling (2022) (1)
Cancer II (2018) (1)
Germinal Center Kinase Regulates The Proliferation and Survival Of Diffuse Large B-Cell Lymphoma (2013) (1)
Inhibition of Phosphatidylinositol-5-Phosphate 4-Kinases (PI5P4Kα and β) Inhibits Proliferation and Radiosensitizes Triple Negative Breast Cancer Cells Harboring p53 Mutations (2015) (1)
Chromatin Accessibility Profiling Reveals Cis-Regulatory Heterogeneity and Novel Transcription Factor Dependencies in Multiple Myeloma (2018) (1)
Abstract 1505: Suppression of triple-negative breast cancer tumorigenesis by targeting cancer stem cells through JNK/Notch1 signaling inhibition (2015) (1)
Resource A Landscape of Pharmacogenomic Interactions in Cancer Graphical Abstract Highlights (2016) (1)
Correction: Evaluation of ERK as a therapeutic target in acute myelogenous leukemia (2020) (1)
Abstract 2809: Pathway dependence on the tyrosine kinase TYK2 in T-cell acute lymphoblastic leukemia (2011) (1)
A new role for the SRC family kinase HCK as a driver of SYK activation in MYD88 mutated lymphomas (2022) (1)
Unleashing cell-intrinsic inflammation as a strategy to kill AML blasts. (2022) (1)
Crystal Structure of MAPK7 (ERK5) with inhibitor (2012) (1)
P089 Identification of the first protein kinase inhibitors that switch macrophages from pro-inflammatory to anti-inflammatory cytokine production (2012) (1)
c-Src kinase domain Thr338Ile mutant in complex with ATPgS (2008) (1)
MEF2C phosphorylation is required for chemotherapy resistance in acute myeloid leukemia (2017) (1)
Abstract 2441: CDK12/13 inhibition cooperates with the Ewing sarcoma oncoprotein EWS/FLI to attenuate homologous recombination repair in Ewing sarcoma cells (2016) (1)
Author Correction: Tuning microtubule dynamics to enhance cancer therapy by modulating FER-mediated CRMP2 phosphorylation (2022) (1)
Development of a Covalent Inhibitor of c-Jun N-Terminal Protein Kinase (JNK) 2/3 with Selectivity over JNK1. (2023) (1)
Crystal structure of Aurora B kinase in complex with a aminothiazole inhibitor (2008) (1)
Discovery of inhibitors that overcome the G1202R ALK Resistance Mutation (2016) (1)
Abstract A12: Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC (2015) (1)
Selective Macrocyclic Inhibitors of DYRK1A/B. (2022) (1)
The combination of FLT3 and SYK kinase inhibitors is toxic to leukaemia cells with CBL mutations (2020) (1)
MYD88 Triggered SYK Activation Promotes BCR Cross-Talk, and Identifies SYK As a Novel Therapeutic Target of Mutated MYD88 Signaling (2018) (1)
Cancer Biology and Signal Transduction PIM Kinases Are Essential for Chronic Lymphocytic Leukemia Cell Survival ( PIM 2 / 3 ) and CXCR 4-Mediated Microenvironmental Interactions ( PIM 1 ) (2014) (1)
CDK12 loss in cancer cells affects DNA damage response genes through premature cleavage and polyadenylation (2019) (1)
Abstract 2757: Discovery and characterization of covalent Pin1 inhibitors targeted to an active site cysteine (2019) (1)
A-770041 reverses paclitaxel and doxorubicin resistance in osteosarcoma cells (2014) (1)
Targeting MYC dependency in ovarian cancer through inhibition of 1 CDK 7 and CDK 12 / 13 2 (1)
A Unified Mechanism of Tyrosine Kinase Regulation by the Gatekeeper Residue. (2007) (1)
STRIPAK directs PP2A activity toward MAP4K4 to promote oncogenic transformation (2019) (1)
MALT1 DEGRADATION FOR THE TREATMENT OF ACTIVATED B‐CELL TYPE DIFFUSE LARGE B‐CELL LYMPHOMA (2021) (1)
ITK degradation to block T cell receptor signaling and overcome therapeutic resistance in T cell lymphomas. (2023) (1)
1 MEF 2 C phosphorylation is required for chemotherapy resistance in acute myeloid leukemia (2017) (0)
Complex between the kinase domain of human ephrin type-a receptor 7 (epha7) and inhibitor alw-ii-49-7 (2008) (0)
Crystal structure of ERK1 covalently bound to SM1-71 (2019) (0)
Chapter 3. Immediate and Selective Control of Protein Abundance Using the dTAG System (2020) (0)
Inhibition of the deubiquitinase USP10 induces degradation of SYK (2020) (0)
LG-47TYPE II RAF INHIBITORS INHIBIT BRAF MUTATIONS AND TRUNCATED FUSIONS IN PEDIATRIC LOW-GRADE GLIOMAS (2016) (0)
Abstract 3408: Targeting cancer cells with potent activators of the PP2A protein phosphatase tumor suppressor (2020) (0)
104 The molecular context of vulnerability for CDK9 suppression in melanoma (2020) (0)
SYK is activated by mutated MYD88 and drives pro-survival signaling in MYD88 driven B-cell lymphomas (2020) (0)
Inhibitors myristate small molecules BCR-ABL and methods of use (2008) (0)
Partitioning of cancer therapeutics in nuclear condensates. (2021) (0)
Targeting transcription in heart failure via CDK7/12/13 inhibition (2022) (0)
Abstract 4454: The AXL tyrosine kinase receptor contributes to ALK-inhibitor resistance in neuroblastoma. (2013) (0)
Inhibition of BCR/ABL-T315I by Dismantling the Hydrophobic Spine. (2008) (0)
Structure of DDB1-DDA1-DCAF15 complex bound to Indisulam and RBM39 (2019) (0)
Crystal structure of MKK7 (MAP2K7) covalently bound with type-II inhibitor SB1-G-23 (2020) (0)
Abstract A25: Dual inhibition of Flt3 and Fes tyrosine kinases potently blocks proliferation of AML cells expressing an active Flt3 mutant. (2015) (0)
Abstract 3644: Identification of existing targeted agents that inhibit NTRK and ROS1 in lung cancer (2015) (0)
HUMAN CYCLIN DEPENDENT KINASE 2 COMPLEXED WITH THE INHIBITOR PURVALANOL B (1999) (0)
Abstract PR04: Targeting super-enhancer driven oncogene transcription through cyclin-dependent kinase inhibitors (2016) (0)
Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase of a Potent and Selective DDR1 Receptor Tyrosine Kinase (2013) (0)
Abstract 1724: Genomic mechanisms of exquisite sensitivity and acquired resistance to everolimus in a patient with anaplastic thyroid carcinoma (2014) (0)
Abstract PR05: Targeting of CDK7 inhibits super-enhancer-associated oncogenic programs in MYCN-amplified tumor cells (2015) (0)
Automated identification of regions of interest in digital images from paraffin sections of human non-small cell lung cancer using GenieTM pattern recognition software. (2011) (0)
Development of Fluorescent Probes for Cancer Cell Lines (2013) (0)
Author response: Dual targeting of salt inducible kinases and CSF1R uncouples bone formation and bone resorption (2021) (0)
Structure of DDB1-DDA1-DCAF15 complex bound to E7820 and RBM39 (2019) (0)
Reciprocal inhibition of PIN1 and APC/CCDH1 controls timely G1/S transition and creates therapeutic vulnerability (2023) (0)
X-ray Crystal Structure of ERK5 (MAPK7) in Complex with a Specific Inhibitor this article openly available. Please share how this access benefits you. Your story matters (2013) (0)
Design and Selection of Small Molecule Inhibitors (2012) (0)
A non-canonical SWI/SNF complex is a synthetic lethal target in cancers driven by BAF complex perturbation (2018) (0)
Crystal structure of MKK7 (MAP2K7) covalently bound with CPT1-70-1 (2020) (0)
Abstract 861: Selective small-molecule kinase inhibitors of the c-Src:FAK complex (2012) (0)
AWARD NUMBER: W81XWH-16-1-0106 TITLE: Fragment-Based Approaches to Enhance GTP Competitive KRAS G12C Inhibitors PRINCIPAL INVESTIGATOR: Kenneth Westover CONTRACTING ORGANIZATION: University of Texas Southwestern Medical Center (2018) (0)
Abstract 1541: Secondary mutations in ALK and resistance to ALK kinase inhibitors (2011) (0)
Triple Degradation of BTK, IKZF1 and IKZF3 in B-Cell Malignancies (2018) (0)
Activity of Plk Inhibitor BI2536 on Myeloma Cells (2008) (0)
Aurora kinase selective inhibitors identified using a Taxol-induced checkpoint sensitivity screen. (2012) (0)
Targeting Cellular , Not Viral , Proteins Immunodeficiency Virus Type 1 by Simplex Virus and Human and Drug-Resistant Strains of Herpes Inhibitors Inhibit Replication of Wild-Type Pharmacological Cyclin-Dependent Kinase (2002) (0)
Crystal Structure of the Jak3 Kinase Domain Covalently Bound to N-(3-(((5-chloro-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)methyl)phenyl)acrylamide (2016) (0)
TYK2-STAT1 Pathway Positively Regulates BCL2 Gene Expression in T-Cell Acute Lymphoblastic Leukemia (2012) (0)
Abstract 1941: Distinct roles of c-Jun N-terminal kinase (JNK) isoforms in skin cancer (2015) (0)
Abstract 955: Combined inhibition of MEK and mTOR pathways is effective inNRAS Q61Kmutant small cell lung cancer (2018) (0)
Small-molecule targeting of brachyury transcription factor addiction in chordoma (2019) (0)
CRISPR-Based Functional Genomics Studies Reveal Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins: Implications for Novel Therapeutics across Diverse Neoplasias (2018) (0)
Identification of Wee1 and IGF-1R As Novel Therapeutic Targets for Mutant RAS-Driven Acute Leukemia By Combinatory Chemical Screens (2014) (0)
Use of FDG-PET for early response assessment of novel EGFR kinase inhibitors in mouse models of lung cancer (2010) (0)
Abstract LB076: Unleashing cell-intrinsic inflammation as a strategy to kill AML blasts (2022) (0)
BORIS promotes chromatin regulatory interactions in treatment-resistant cancer cells (2019) (0)
Functional Characterization of E3 Ligases and Their Regulators: Therapeutic Implications for Development of New Proteolysis-Targeting Chimeric Degraders of Oncoproteins (2019) (0)
Abstract 3744: Single-cell analysis of adaptive resistance and fractional responses of melanoma cells to RAF/MEK inhibition (2015) (0)
1 TYK 2-STAT 1-BCL 2 Pathway Dependence in T-Cell Acute Lymphoblastic Leukemia (2013) (0)
Abstract 1358: Discovery and optimization of potent and selective benzonaphthyridinone analogs as dual mTOR/ATR small molecular inhibitors for treatment of cancer (2011) (0)
Abstract 5487: Identification of super-enhancer-associated cancer genes provides novel therapeutic targets in adult T-cell leukemia/lymphoma (2017) (0)
Abstract 1118: Synthetic lethality of CDK12 inhibition in tumors with EWS/FLI rearrangements (2017) (0)
Targeting transcription cycles in cancer (2021) (0)
Studies of TAK 1-centered polypharmacology with novel covalent TAK 1 inhibitors (2017) (0)
EML4-ALK fusion gene and sensitivity to an ALK kinase inhibitor in lung cancer (2008) (0)
Abstract 1222: Developing kinase inhibitors with polypharmacological profiles for the treatment of resistant cancers (2017) (0)
SIKs control osteocyte responses to parathyroid hormone Citation (2016) (0)
Crystal structure of ERK2 covalently bound to SM1-71 (2019) (0)
Structure-Based Design of Y-Shaped Covalent TEAD Inhibitors. (2023) (0)
Shoghag upon Binding to an Allosteric Inhibitor Localizes to the Endoplasmic Reticulum-Myristoylated c-Abl Tyrosine Kinase N Mechanisms of Signal Transduction : (2009) (0)
Abstract 3904: Inhibition of the ERK5 pathway as a novel approach to target human chronic myeloid leukemia stem cells (2017) (0)
Correction to "Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one Scaffold". (2020) (0)
Selectivity and binding kinetics of mTOR inhibitors 2 (2011) (0)
Selective Mediator dependence of cell-type-specifying transcription (2020) (0)
Aberrant Phosphorylation of MEF2C Is Dispensable for Hematopoiesis, and Induces Chemotherapy Resistance and Susceptibility to MARK Kinase Inhibition Therapy in Acute Myeloid Leukemia (2016) (0)
Abstract 3426: Catalytic degraders effectively address kinase site mutations in EML-ALK oncogenic fusions (2023) (0)
Genomic and Proteomic Analysis of Primary Chemoresistance and Induction Failure in Acute Myeloid Leukemia (2015) (0)
Transcriptional Antagonism by CDK8 Inhibition Improves Therapeutic Efficacy of MEK Inhibitors. (2022) (0)
Depletion of creatine phosphagen energetics with a covalent creatine kinase inhibitor. (2023) (0)
Molecular Cancer apeutics apeutic Discovery overy and Characterization of Novel Mutant Ther 3 Kinase Inhibitors (2010) (0)
Transcription Regulation Targeting in Peripheral T Cell Lymphomas Induces Apoptosis and Sensitization to BCL2 Inhibitors (2014) (0)
Abstract A178: Structure guided development of irreversible inhibitors for TAK1 (2015) (0)
Correction to Discovery of Immunologically Inspired Small Molecules That Target the Viral Envelope Protein. (2019) (0)
786: The mitogen-activated protein kinase ERK5 regulates the development and growth of hepatocellular carcinoma (2014) (0)
Targeting Vulnerabilities in Successive Cell Cycle Stages to Induce Death of PI3K-Activated Basal-Like Breast Cancer Cells (2018) (0)
mTOR , ATM and ATR Characterization of Torin 2 , an ATP-competitive inhibitor of (2013) (0)
Abstract 2834: Genomewide CRISPR studies of sequential treatment with CRBN-based degronimids: Insights into the molecular evolution of treatment resistance in myeloma and beyond (2018) (0)
Author response: Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13 (2018) (0)
Abstract 2935: The ATP-competitive mTOR inhibitor Torin2 enhances sensitivity of the ALK F1174L mutation to crizotinib in neuroblastoma (2012) (0)
Abstract 15: Suppression of adaptive responses to targeted therapies by transcriptional inhibition (2017) (0)
Abstract GS3-10: Partitioning of cancer therapeutics in nuclear condensates (2021) (0)
Compositions and immunosuppressive compounds (2004) (0)
Quantitative assessment of tumour infiltrating lymphocytes using GenieTM pattern recognition software for the separate analysis of tumour versus stroma in head and neck squamous cell carcinoma (HNSCC) improves biomarker reproducibility (2011) (0)
Cover Picture: Chemical Interrogation of the Malaria Kinome (ChemBioChem 13/2014) (2014) (0)
Author response: STRIPAK directs PP2A activity toward MAP4K4 to promote oncogenic transformation of human cells (2020) (0)
Elevated stromal Foxp3+ regulatory T cells combined with low density CD8+ cytotoxic T cells are associated with colorectal metastatic tumour progression (2011) (0)
MICROTUBULE STABILIZING DRUGS Paclitaxel and Docetaxel Paclitaxel (2006) (0)
A New Role for the SRC Family Member HCK As a Driver of BCR/SYK Signaling in MYD88 Mutated Lymphomas (2021) (0)
Abstract B13: FGFR2 as a therapeutic target in squamous cell lung carcinoma (2012) (0)
Small Molecule Inhibitors of USP1 Target ID1 Degradation in Leukemic Cells and Cause Cytotoxicity (2013) (0)
Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors (2020) (0)
BET Bromodomain Protein s Function as Master Transcription Elongation Factors Independent of CDK 9 Recruitment Graphical (2017) (0)
Abstract 1420: Chemoproteomic Profiling Surveys the Degradable Proteome (2023) (0)
705 Cyclin-dependent kinase 9 (CDK9) as a therapeutic target in uveal and triple-wild type melanoma (2019) (0)
Human Polo-like Kinase Inhibitors as Antiplasmodials. (2023) (0)
GTP-Competitive Inhibitors of RAS Family Members (2017) (0)
Redirecting the Neo-Substrate Specificity of Cereblon-Targeting PROTACs to Helios. (2022) (0)
Abstract 2195: A high-throughput chemical screen identifies synergistic activity between crizotinib and transcriptional CDK inhibitors in ALK-mutated neuroblastoma (2015) (0)
Structure of Maternal Embryonic Leucine Zipper Kinase (2017) (0)
Targeting the Dark Lipid Kinase PIP4K2C with a Potent and Selective Binder and Degrader. (2023) (0)
Compounds and compositions as inhibitors of protein kinases. (2006) (0)
Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model (2017) (0)
Shining light on reprogramming Tregs for cancer therapy. (2023) (0)
Targeting Myddosome Self-Assembly in Waldenstrom's Macroglobulinemia (2015) (0)
Development of a Selective CDK 7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype Graphical (2019) (0)
Erk 5 Is a Key Regulator of Naive-Primed Transition and Embryonic Stem Cell Identity Graphical (0)
Rewiring Cancer Drivers to Activate Apoptosis (2022) (0)
225 Diversity in Individual Src-family Kinase Regulation: Opportunities for Selective Inhibitor Discovery (2012) (0)
Abstract 5578: Quantitative kinase inhibitor profiling in native cell and tissue extracts (2010) (0)
Abstract 3683: Small molecule inhibitors of the Fes non-receptor tyrosine kinase (2010) (0)
Abstract GS1-07: Treatment persistence of residual breast tumors through an embryonic diapause-like cancer cell state with suppressed myc activity (2021) (0)
Using Small Molecules To Identify Critical Signaling Pathways Of Mutant N-RAS In Acute Leukemia Cells (2013) (0)
Abstract LB-C24: Resistance to ALK inhibition is associated with enhanced BRD4 dependence in ALK-mutated MYCN-amplified neuroblastoma (2015) (0)
Stem Cell Repor ts Targeting the Extracellular Signal-Regulated Kinase 5 Pathway to Suppress Human Chronic Myeloid Leukemia Stem Cells (2018) (0)
Genome wide chromatin accessibility profiling identifies chromatin signatures and novel transcription factor dependencies in multiple myeloma (2019) (0)
Abstract 890: TGFâ upregulation mediates growth retardation in EGFR T790M mutant non-small cell lung cancer (2016) (0)
Abstract B180: Multi-targeted tyrosine kinase inhibitors potently suppress FLT3-ITD+ AML cell growth (2015) (0)
A Unique N-Phenylbenzamide Inhibitor Targeting Non-Receptor Tyrosine Kinases Potently Suppresses AML Cell Growth In Vitro and In Vivo (2017) (0)
Crystal structure of Aurora-A in complex with FMF-03-145-1 (compound 2) (2017) (0)
2,4-di (phenylamino) pyrimidines useful in the treatment of neoplastic diseases, inflammatory disorders and disorders of the immune system (2004) (0)
Development and characterization of selective FAK inhibitors and PROTACs with in vivo activity. (2023) (0)
EPHA2BlockadeOvercomesAcquired Resistance to EGFR Kinase Inhibitors in Lung Cancer (2016) (0)
Targeting Salt-Inducible Kinase 3 As a Therapeutic Approach for Acute Myeloid Leukemia (2019) (0)
Combined inhibition of mTOR and PIKKs exploits replicative and checkpoint vulnerabilities to induce death of PI3K-activated triple-negative breast cancer cells (2019) (0)
DCA promotes a novel tolerogenic program in CD4+ T cells by inhibiting CDK8 (2019) (0)
Abstract PR04: Degradation of leukemia oncogenes: A novel approach to therapy of leukemia (2017) (0)
Targeted Kinase Degradation via the KLHDC2 Ubiquitin E3 Ligase (2022) (0)
Small Molecule Inhibitors: Design and Selection (2008) (0)
Abstract 2086: Dual inhibitors of Flt3 and c-Fest tyrosine kinases potently inhibit proliferation of AML cells expressing an active Flt3 mutant. (2013) (0)
Development of PRPK Directed Phthalimides (2021) (0)
Crystal Structure of Human Dual Specificity Protein Kinase (TTK) in complex with a pyrimido-diazepin ligand (2009) (0)
Citron Rho-Interacting Serine/Threonine kinase (CIT) Is a Novel Therapeutic Target in Multiple Myeloma Cells (2014) (0)
Fibroblast Growth Factor Receptor 1–TransformedMammary Epithelial Cells Are Dependent on RSK Activity for Growth and Survival (2009) (0)
Development and Repurposing of Small-Molecule Kinase Inhibitors to Target Novel Leukemogenic TNK2 Mutations (2014) (0)
Abstract LB-125: Selective inhibition of CDK7 targets MYCN-driven transcriptional amplification in neuroblastoma (2014) (0)
Development of potent and selective degraders of PI5P4Kγ. (2022) (0)
Targeting T-ALL Cells with Potent Activators of the PP2A Protein Phosphatase Tumor Suppressor (2019) (0)
Author Correction: Tuning microtubule dynamics to enhance cancer therapy by modulating FER-mediated CRMP2 phosphorylation (2018) (0)
Abstract 750: JNK-IN-8: a novel covalent inhibitor targeting JNK signaling in triple-negative breast cancer (2014) (0)
Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2 (2021) (0)
Structure of DDB1-DDA1-DCAF15 complex bound to tasisulam and RBM39 (2019) (0)
Effect of Covalent TAK1 Inhibitors on the Viability of Pancreatic, Renal and Colon Cancer Cells (2016) (0)
Abstract B50: Targeting EWS/FLI fusion oncoprotein stability/degradation in Ewing sarcoma (2020) (0)
Chabner Colloquium: Answering the Big Questions in Cancer Research & 2016 STO Annual Meeting (Boston, MA: November 11-12, 2016) (2016) (0)
USP9X mediates an acute adaptive response to MAPK suppression in pancreatic cancer but creates multiple actionable therapeutic vulnerabilities (2023) (0)
Waldenström macroglobulinemia lymphoplasmacytic cells by activation of Bruton tyrosine kinase in A mutation in MYD88 (L265P) supports the survival of (2014) (0)
Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions. (2023) (0)
Molecular markers of myeloma cell sensitivity vs. resistance to heterobifunctional degraders of oncoproteins: therapeutic implications. (2019) (0)
Covalent GTP-competitive inhibitors of KRAS G12C: Guanosine bisphosphonate Analogs (2017) (0)
Abstract 790: A high-throughput chemical screen identifies synergistic activity between neurotransmitter receptor inhibitors and crizotinib in ALK-mutated neuroblastoma (2014) (0)
Abstract 2852: Torin2 suppresses ionizing radiation induced DNA damage repair (2015) (0)
Abstract 3424: Template-assisted covalent modification of DCAF16 enables BRD4 molecular glue degraders (2023) (0)
Targeting chronic myeloid leukemia stem cells with ERK5 pathway inhibitors. (2018) (0)
MEK5-ERK5 inhibitors target chronic myeloid leukemia stem cells and in combination with imatinib reduce the expression of stem cell genes (2016) (0)
CRISPR studies identify genes preferentially essential for myeloma cells vs. other neoplasias: implications for future therapies selective against MM (2019) (0)
Human EphA3 kinase domain in complex with inhibitor AWL-II-38.3 (2008) (0)
Abstract B74: Combined inhibition of ALK and CDKs involved in transcriptional regulation is synergistic in ALK-mutated neuroblastoma (2015) (0)
Supplemental Information Small-Molecule Inhibitors of the c-Fes Protein-Tyrosine Kinase (2012) (0)
# 2 TP 53 MUTATION IS A BIOMARKER FOR PROGNOSIS IN TRIPLE-NEGATIVE BREAST CANCER PATIENTS TREATED WITH POST-NEOADJUVANT CISPLATIN (2016) (0)
Abstract 5605: Pharmacologic inhibition of EphA2 in NRAS and BRAF mutant melanomas. (2013) (0)
Optimization of experimental antimitotic agents: classical and combinatorial methods. (2003) (0)
Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders (2023) (0)
Deciphering the Critical Pathways of Mutant N-RAS in AML Using Small Molecule Inhibitors. (2012) (0)
Correction: Fragment-based covalent ligand discovery (2021) (0)
A chemistry-based approach to identify factors involved in spindle assembly (1999) (0)
Abstract LB216: Targeted brachyury degradation disrupts a highly specific autoregulatory program controlling chordoma cell identity (2021) (0)
Abstract B165: Abl kinase myristate‐site inhibitor, mechanism and application (2009) (0)
Advancing targeted protein degrader discovery by measuring cereblon engagement in cells. (2023) (0)
Characterization of a novel cdk inhibitor using Xenopus egg extracts. (1998) (0)
Abstract A057: Therapeutic efficacy of selective CDK7 inhibition in pancreatic cancer mediated by induction of R-loop formation, DNA replication stress and genomic instability (2022) (0)
The Salt-Inducible Kinase inhibitor YKL-05-099 suppresses MEF2C function and acute myeloid leukemia progression in vivo (2019) (0)
Crystal structure of human Feline Sarcoma Viral Oncogene Homologue (v-FES)in complex with TAE684 (2012) (0)
PO-099 Targeting the mitogen activated protein kinase ERK5 in human melanoma (2018) (0)
Structural and atropisomeric factors governing the selectivity profile of pyrimido-benzodiazipinones as inhibitors of kinases and bromo- domains (2019) (0)
chicken c-Src kinase domain in complex with ATPgS (2008) (0)
Crystal structure of MKK7 (MAP2K7) covalently bound with type-II inhibitor TL10-105 (2020) (0)
Multi-omic profiling of breast cancer cells uncovers stress MAPK-associated sensitivity to AKT degradation (2022) (0)
Targeted degradation of BRD 9 reverses oncogenic gene 1 expression in synovial sarcoma 2 3 (0)
Abstract B103: Torin2 and related analogs exploit replicative and checkpoint vulnerabilities to induce death of triple-negative breast cancer cells (2019) (0)
Abstract PR07: Crystal structure of K-Ras G12C bound to an active site inhibitor (2014) (0)
The CDK8 inhibitor DCA promotes a tolerogenic chemical immunophenotype in CD4+ T cells via a novel CDK8-GATA3-FOXP3 pathway (2019) (0)
Supplemental Information Activation of HIPK 2 Promotes ER Stress-Mediated Neurodegeneration in Amyotrophic Lateral Sclerosis (2016) (0)
Application of GenieTM Pattern Recognition Software for the Automated Analysis of Immunohistochemical (IHC) Markers in Preclinical Xenograft Models. (2011) (0)
CDK7 controls E2F- and MYC-driven proliferative and metabolic vulnerabilities in multiple myeloma. (2023) (0)
Abstract C48: Defining mechanisms of adaptation to KRAS G12C inhibitors: Using quantitative proteomics to design combinatorial strategies in pancreatic cancer (2019) (0)
The rise of molecular glues and bifunctional compounds (2022) (0)

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