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Nathanael Gray, PhD


Researcher

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Researcher

  • Nancy Lurie Marks Professor of Biological Chemistry and Molecular Pharmacology, Harvard Medical School

Contact Information

  • Office Phone Number617-582-8590
  • Fax617-582-8615

Bio

Nathanael Gray received his PhD in chemistry from the University of California at Berkeley in 1999. He then moved to the Genomics Institute of the Novartis Research Foundation in San Diego, where after serving as a staff scientist and group leader of kinase inhibitor chemistry, he was named director of biological chemistry in 2001. Dr. Gray recently joined the faculty of Harvard Medical School and DFCI to continue his research using synthetic chemistry and functional small molecule discovery to modulate biological pathways important in cancer.

Research

Synthetic Chemistry/Functional Small Molecule Discovery

Our lab is interested in the following general questions: 1. How can small molecule inhibitors with selectivity towards a desired wild-type or drug-resistant kinase be efficiently developed? 2. How can we use kinase inhibitors to dissect the molecular wiring of signaling pathways? 3. What are the most efficient ways to develop small molecule modulators for protein targets for which no ligand is currently known? 4. How do you develop a small molecule modulator for biological pathways for which very little is known? 5. What are new methods for identifying the biological targets for small molecules of unknown mechanism? Synthetic Chemistry: Our lab uses synthetic organic chemistry to make combinatorial gene-family targeted libraries. We typically base the libraries on close variants of scaffolds that have been previously shown to have interesting biological activity (so called 'privileged scaffolds'). We use solution and solid-phase chemistry and employ 'directed-sorting' technology to enable efficient library production. We also perform medicinal chemistry to improve the potency, cellular activity, specificity, stability and pharmacological properties of our initial 'lead' compounds. Functional Small Molecule Discovery: Following synthesis of new compounds, we use three distinct but complementary approaches to discover and optimize their biological function: (1) target-based biochemical screening (2) functional target-based cellular assays and (3) cellular or organismal 'phenotypic' screening. Target-based screening supported by cellular assays that precisely monitor the activity of interest and that can guide chemical optimization is the most direct means to obtain functional inhibitors. The target-based cellular screens present a significant advantage over biochemical assays because the kinases are expressed in an appropriate cellular context allowing compounds to be identified that may possess a number of distinct mechanisms including: direct inhibition of the active kinase, binding to the inactive form of the kinase, inhibiting activating phosphorylations, or interacting with negative regulators. We are in the process of creating a battery of such cellular assays that will allow us to more fully annotate the kinase selectivity of a given compound which can then be used as a chemical probe in various biological systems. In contrast, phenotypic screening provides a means to interrogate a pathway in an unbiased fashion with small molecules. Provided that the molecular target(s) of the compound can be identified (usually by affinity chromatography, genetic complementation, or expression profiling), phenotypic screening can deliver new biological insight in addition to yielding useful small molecules. For more information, please visit our Web site at http://research.dfci.harvard.edu/gray_lab/home.htm.

The Cyclin-Dependent Kinase 8 (CDK8) Inhibitor DCA Promotes a Tolerogenic Chemical Immunophenotype in CD4+ T Cells via a Novel CDK8-GATA3-FOXP3 Pathway. Mol Cell Biol. 2021 08 24; 41(9):e0008521.
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Targeting Pin1 renders pancreatic cancer eradicable by synergizing with immunochemotherapy. Cell. 2021 Sep 02; 184(18):4753-4771.e27.
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COVID symptoms, testing, shielding impact on patient-reported outcomes and early vaccine responses in individuals with multiple myeloma. Br J Haematol. 2021 Aug 02.
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TRIM8 modulates the EWS/FLI oncoprotein to promote survival in Ewing sarcoma. Cancer Cell. 2021 Jul 22.
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Exploring Ligand-Directed N-Acyl-N-alkylsulfonamide-Based Acylation Chemistry for Potential Targeted Degrader Development. ACS Med Chem Lett. 2021 Aug 12; 12(8):1302-1307.
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Selective degradation-inducing probes for studying cereblon (CRBN) biology. RSC Med Chem. 2021 Aug 18; 12(8):1381-1390.
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Dual targeting of salt inducible kinases and CSF1R uncouples bone formation and bone resorption. Elife. 2021 06 23; 10.
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The HCK/BTK inhibitor KIN-8194 is active in MYD88 driven lymphomas and overcomes mutated BTKCys481 ibrutinib resistance. Blood. 2021 06 16.
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Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2. Angew Chem Int Ed Engl. 2021 07 12; 60(29):15905-15911.
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Cancer stem cell marker DCLK1 reprograms small extracellular vesicles toward migratory phenotype in gastric cancer cells. Proteomics. 2021 Jul; 21(13-14):e2000098.
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Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 06; 17(6):711-717.
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The PP2A-Integrator-CDK9 axis fine-tunes transcription and can be targeted therapeutically in cancer. Cell. 2021 Jun 10; 184(12):3143-3162.e32.
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ULK1 inhibition overcomes compromised antigen presentation and restores antitumor immunity in LKB1 mutant lung cancer. Nat Cancer. 2021 May; 2(5):503-514.
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Generation of a chemical genetic model for JAK3. Sci Rep. 2021 May 12; 11(1):10093.
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Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo. Nat Chem Biol. 2021 09; 17(9):954-963.
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Inhibition of CDK4/6 promotes CD8 T-cell memory formation. Cancer Discov. 2021 May 03.
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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. Eur J Med Chem. 2021 Oct 05; 221:113481.
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Discovery and resistance mechanism of a selective CDK12 degrader. Nat Chem Biol. 2021 06; 17(6):675-683.
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Correction: Fragment-based covalent ligand discovery. RSC Chem Biol. 2021 Apr 01; 2(2):670-671.
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Fragment-based covalent ligand discovery. RSC Chem Biol. 2021 Apr 01; 2(2):354-367.
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Targeting oncoproteins with a positive selection assay for protein degraders. Sci Adv. 2021 Feb; 7(6).
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Mammalian cell proliferation requires noncatalytic functions of O-GlcNAc transferase. Proc Natl Acad Sci U S A. 2021 01 26; 118(4).
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Targeted brachyury degradation disrupts a highly specific autoregulatory program controlling chordoma cell identity. Cell Rep Med. 2021 Jan 19; 2(1):100188.
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The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification. Int J Mol Sci. 2021 Jan 08; 22(2).
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An Embryonic Diapause-like Adaptation with Suppressed Myc Activity Enables Tumor Treatment Persistence. Cancer Cell. 2021 Feb 08; 39(2):240-256.e11.
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Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins. Cell Rep. 2021 01 05; 34(1):108532.
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Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor. ACS Med Chem Lett. 2021 Jan 14; 12(1):30-38.
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Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development. Cell. 2020 12 10; 183(6):1714-1731.e10.
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Genomic and pathological heterogeneity in clinically diagnosed small cell lung cancer in never/light smokers identifies therapeutically targetable alterations. Mol Oncol. 2021 01; 15(1):27-42.
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Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma. J Clin Invest. 2020 11 02; 130(11):5875-5892.
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Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma. ACS Med Chem Lett. 2020 Nov 12; 11(11):2238-2243.
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Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library. ACS Chem Biol. 2020 10 16; 15(10):2722-2730.
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Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules. Nat Commun. 2020 09 18; 11(1):4687.
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Discovery of Covalent MKK4/7 Dual Inhibitor. Cell Chem Biol. 2020 12 17; 27(12):1553-1560.e8.
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Correction: Evaluation of ERK as a therapeutic target in acute myelogenous leukemia. Leukemia. 2020 Sep; 34(9):2543.
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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". J Med Chem. 2020 Sep 10; 63(17):10088.
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Catalytic Domain Plasticity of MKK7 Reveals Structural Mechanisms of Allosteric Activation and Diverse Targeting Opportunities. Cell Chem Biol. 2020 10 15; 27(10):1285-1295.e4.
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Repurposing of Kinase Inhibitors for Treatment of COVID-19. Pharm Res. 2020 Aug 10; 37(9):167.
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Chemical Biology Toolkit for DCLK1 Reveals Connection to RNA Processing. Cell Chem Biol. 2020 10 15; 27(10):1229-1240.e4.
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Discovery of a series of benzopyrimidodiazepinone TNK2 inhibitors via scaffold morphing. Bioorg Med Chem Lett. 2020 10 01; 30(19):127456.
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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. J Med Chem. 2020 07 23; 63(14):7817-7826.
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Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations. Angew Chem Int Ed Engl. 2020 08 17; 59(34):14481-14489.
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Current therapies under investigation for COVID-19: potential COVID-19 treatments. Can J Physiol Pharmacol. 2020 Aug; 98(8):483-489.
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Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13. J Med Chem. 2020 07 09; 63(13):6708-6726.
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Partitioning of cancer therapeutics in nuclear condensates. Science. 2020 06 19; 368(6497):1386-1392.
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Extracellular-Regulated Protein Kinase 5-Mediated Control of p21 Expression Promotes Macrophage Proliferation Associated with Tumor Growth and Metastasis. Cancer Res. 2020 08 15; 80(16):3319-3330.
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Increased lysosomal biomass is responsible for the resistance of triple-negative breast cancers to CDK4/6 inhibition. Sci Adv. 2020 Jun; 6(25):eabb2210.
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Development of CDK2 and CDK5 Dual Degrader TMX-2172. Angew Chem Int Ed Engl. 2020 08 10; 59(33):13865-13870.
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Identification of a potent and selective covalent Pin1 inhibitor. Nat Chem Biol. 2020 09; 16(9):979-987.
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Selective Mediator dependence of cell-type-specifying transcription. Nat Genet. 2020 07; 52(7):719-727.
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Salt-inducible kinase 1 maintains HDAC7 stability to promote pathologic cardiac remodeling. J Clin Invest. 2020 06 01; 130(6):2966-2977.
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Structure and Characterization of a Covalent Inhibitor of Src Kinase. Front Mol Biosci. 2020; 7:81.
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CDK13 cooperates with CDK12 to control global RNA polymerase II processivity. Sci Adv. 2020 May; 6(18).
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CDK13 cooperates with CDK12 to control global RNA polymerase II processivity. Sci Adv. 2020 May; 6(18):eaaz5041.
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Tubulin Resists Degradation by Cereblon-Recruiting PROTACs. Cells. 2020 04 27; 9(5).
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Discovery and Structure-Activity Relationship Study of (Z)-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors. J Med Chem. 2020 05 14; 63(9):4880-4895.
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Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2. Cell. 2020 04 30; 181(3):702-715.e20.
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Discovery of a selective inhibitor of doublecortin like kinase 1. Nat Chem Biol. 2020 06; 16(6):635-643.
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Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface. ACS Med Chem Lett. 2020 Jun 11; 11(6):1269-1273.
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Defining and Targeting Adaptations to Oncogenic KRASG12C Inhibition Using Quantitative Temporal Proteomics. Cell Rep. 2020 03 31; 30(13):4584-4599.e4.
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Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors. Nat Commun. 2020 03 13; 11(1):1383.
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Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors. Cell Chem Biol. 2020 05 21; 27(5):525-537.e6.
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Correction: An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem. 2020 Feb 28; 295(9):2886.
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A Quantitative Tissue-Specific Landscape of Protein Redox Regulation during Aging. Cell. 2020 03 05; 180(5):968-983.e24.
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Light-induced control of protein destruction by opto-PROTAC. Sci Adv. 2020 02; 6(8):eaay5154.
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Inhibition of the deubiquitinase USP10 induces degradation of SYK. Br J Cancer. 2020 04; 122(8):1175-1184.
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SYK is activated by mutated MYD88 and drives pro-survival signaling in MYD88 driven B-cell lymphomas. Blood Cancer J. 2020 01 31; 10(1):12.
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Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine. J Med Chem. 2020 02 27; 63(4):1624-1641.
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Effects of the multi-kinase inhibitor midostaurin in combination with chemotherapy in models of acute myeloid leukaemia. J Cell Mol Med. 2020 03; 24(5):2968-2980.
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The combination of FLT3 and SYK kinase inhibitors is toxic to leukaemia cells with CBL mutations. J Cell Mol Med. 2020 02; 24(3):2145-2156.
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Treatment-Induced Tumor Dormancy through YAP-Mediated Transcriptional Reprogramming of the Apoptotic Pathway. Cancer Cell. 2020 01 13; 37(1):104-122.e12.
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STRIPAK directs PP2A activity toward MAP4K4 to promote oncogenic transformation of human cells. Elife. 2020 Jan 08; 9.
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Benzopyrimidodiazepinone inhibitors of TNK2. Bioorg Med Chem Lett. 2020 02 15; 30(4):126948.
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Salt-inducible kinase inhibition suppresses acute myeloid leukemia progression in vivo. Blood. 2020 01 02; 135(1):56-70.
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A broad-spectrum antiviral molecule, QL47, selectively inhibits eukaryotic translation. J Biol Chem. 2020 02 07; 295(6):1694-1703.
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Exploring Targeted Degradation Strategy for Oncogenic KRASG12C. Cell Chem Biol. 2020 01 16; 27(1):19-31.e6.
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CDK7 Inhibition Potentiates Genome Instability Triggering Anti-tumor Immunity in Small Cell Lung Cancer. Cancer Cell. 2020 01 13; 37(1):37-54.e9.
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Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling. Cell Chem Biol. 2020 01 16; 27(1):66-73.e7.
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Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. Cell Syst. 2020 01 22; 10(1):66-81.e11.
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Development and Characterization of a Wee1 Kinase Degrader. Cell Chem Biol. 2020 01 16; 27(1):57-65.e9.
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Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15. Nat Chem Biol. 2020 01; 16(1):7-14.
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Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors. ACS Med Chem Lett. 2020 Mar 12; 11(3):346-352.
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Correction to Discovery of Immunologically Inspired Small Molecules That Target the Viral Envelope Protein. ACS Infect Dis. 2019 Dec 13; 5(12):2176.
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Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors. ACS Med Chem Lett. 2019 Nov 14; 10(11):1549-1553.
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A kinase-independent role for CDK8 in BCR-ABL1+ leukemia. Nat Commun. 2019 10 18; 10(1):4741.
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Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation. Cell Chem Biol. 2019 11 21; 26(11):1486-1500.
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Synthetic Lethal Interaction of SHOC2 Depletion with MEK Inhibition in RAS-Driven Cancers. Cell Rep. 2019 10 01; 29(1):118-134.e8.
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Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold. ACS Med Chem Lett. 2019 Oct 10; 10(10):1443-1449.
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Evaluation of ERK as a therapeutic target in acute myelogenous leukemia. Leukemia. 2020 02; 34(2):625-629.
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BORIS promotes chromatin regulatory interactions in treatment-resistant cancer cells. Nature. 2019 08; 572(7771):676-680.
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Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations. Nat Commun. 2019 08 01; 10(1):3468.
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Pharmacological enhancement of KCC2 gene expression exerts therapeutic effects on human Rett syndrome neurons and Mecp2 mutant mice. Sci Transl Med. 2019 07 31; 11(503).
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Comparison of effects of midostaurin, crenolanib, quizartinib, gilteritinib, sorafenib and BLU-285 on oncogenic mutants of KIT, CBL and FLT3 in haematological malignancies. Br J Haematol. 2019 11; 187(4):488-501.
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Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14. Bioorg Med Chem Lett. 2019 08 01; 29(15):1985-1993.
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Quinoline and thiazolopyridine allosteric inhibitors of MALT1. Bioorg Med Chem Lett. 2019 07 15; 29(14):1694-1698.
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What It Takes to Improve a First-Generation Inhibitor to a Second- or Third-Generation Small Molecule. Am Soc Clin Oncol Educ Book. 2019 Jan; 39:196-205.
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JNK2 Is Required for the Tumorigenic Properties of Melanoma Cells. ACS Chem Biol. 2019 07 19; 14(7):1426-1435.
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Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. Cancer Discov. 2019 07; 9(7):926-943.
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BCL2 Amplicon Loss and Transcriptional Remodeling Drives ABT-199 Resistance in B Cell Lymphoma Models. Cancer Cell. 2019 05 13; 35(5):752-766.e9.
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CDK12 loss in cancer cells affects DNA damage response genes through premature cleavage and polyadenylation. Nat Commun. 2019 04 15; 10(1):1757.
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Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome. Cell Chem Biol. 2019 06 20; 26(6):818-829.e9.
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Cheminformatics Tools for Analyzing and Designing Optimized Small-Molecule Collections and Libraries. Cell Chem Biol. 2019 05 16; 26(5):765-777.e3.
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Peptide-based covalent inhibitors of MALT1 paracaspase. Bioorg Med Chem Lett. 2019 06 01; 29(11):1336-1339.
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Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6. Angew Chem Int Ed Engl. 2019 05 06; 58(19):6321-6326.
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Discovery of Covalent CDK14 Inhibitors with Pan-TAIRE Family Specificity. Cell Chem Biol. 2019 06 20; 26(6):804-817.e12.
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Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models. Elife. 2019 03 25; 8.
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Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype. Cell Chem Biol. 2019 06 20; 26(6):792-803.e10.
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Coordinating Tissue Regeneration Through Transforming Growth Factor-ß Activated Kinase 1 Inactivation and Reactivation. Stem Cells. 2019 06; 37(6):766-778.
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A multitargeted probe-based strategy to identify signaling vulnerabilities in cancers. J Biol Chem. 2019 05 24; 294(21):8664-8673.
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Identification of small molecule inhibitors targeting the Zika virus envelope protein. Antiviral Res. 2019 04; 164:147-153.
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Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor-associated kinase 4 (IRAK4). J Biol Chem. 2019 03 22; 294(12):4511-4519.
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Small-molecule targeting of brachyury transcription factor addiction in chordoma. Nat Med. 2019 02; 25(2):292-300.
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Small Molecules Targeting the Flavivirus E Protein with Broad-Spectrum Activity and Antiviral Efficacy in Vivo. ACS Infect Dis. 2019 03 08; 5(3):460-472.
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Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML. Cell Chem Biol. 2019 02 21; 26(2):300-306.e9.
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A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 01 09; 141(1):191-203.
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Bruton tyrosine kinase degradation as a therapeutic strategy for cancer. Blood. 2019 02 28; 133(9):952-961.
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Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma. Elife. 2018 11 15; 7.
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Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13. Elife. 2018 11 13; 7.
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A non-canonical SWI/SNF complex is a synthetic lethal target in cancers driven by BAF complex perturbation. Nat Cell Biol. 2018 12; 20(12):1410-1420.
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A High-Throughput Immune-Oncology Screen Identifies EGFR Inhibitors as Potent Enhancers of Antigen-Specific Cytotoxic T-lymphocyte Tumor Cell Killing. Cancer Immunol Res. 2018 12; 6(12):1511-1523.
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Targeting the Extracellular Signal-Regulated Kinase 5 Pathway to Suppress Human Chronic Myeloid Leukemia Stem Cells. Stem Cell Reports. 2018 10 09; 11(4):929-943.
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First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia. J Med Chem. 2018 09 27; 61(18):8353-8373.
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Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-benzodiazipinones as Inhibitors of Kinases and Bromodomains. ACS Chem Biol. 2018 09 21; 13(9):2438-2448.
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Discovery of Immunologically Inspired Small Molecules That Target the Viral Envelope Protein. ACS Infect Dis. 2018 09 14; 4(9):1395-1406.
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Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors. J Med Chem. 2018 09 13; 61(17):7560-7572.
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Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor. Angew Chem Int Ed Engl. 2018 09 03; 57(36):11629-11633.
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Specific covalent inhibition of MALT1 paracaspase suppresses B cell lymphoma growth. J Clin Invest. 2018 10 01; 128(10):4397-4412.
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BMX-Mediated Regulation of Multiple Tyrosine Kinases Contributes to Castration Resistance in Prostate Cancer. Cancer Res. 2018 09 15; 78(18):5203-5215.
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Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance. Cell. 2018 07 12; 174(2):300-311.e11.
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How small-molecule inhibitors of dengue-virus infection interfere with viral membrane fusion. Elife. 2018 07 12; 7.
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Targeting chronic myeloid leukemia stem cells with ERK5 pathway inhibitors. J Biol Regul Homeost Agents. 2018 Jul-Aug; 32(4 Suppl. 1):36.
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Inhibition of Flaviviruses by Targeting a Conserved Pocket on the Viral Envelope Protein. Cell Chem Biol. 2018 08 16; 25(8):1006-1016.e8.
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Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 07; 14(7):706-714.
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Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo. ACS Chem Biol. 2018 06 15; 13(6):1551-1559.
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Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). J Med Chem. 2018 05 10; 61(9):4249-4255.
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RAS-MAPK Reactivation Facilitates Acquired Resistance in FGFR1-Amplified Lung Cancer and Underlies a Rationale for Upfront FGFR-MEK Blockade. . 2018 07; 17(7):1526-1539.
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It Takes Two To Target: A Study in KRAS Dimerization. Biochemistry. 2018 04 24; 57(16):2289-2290.
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The dTAG system for immediate and target-specific protein degradation. Nat Chem Biol. 2018 05; 14(5):431-441.
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Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8. ACS Med Chem Lett. 2018 Jun 14; 9(6):540-545.
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Kinase inhibitors: the road ahead. Nat Rev Drug Discov. 2018 05; 17(5):353-377.
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Correction: MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells. Elife. 2018 03 12; 7.
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Myeloid ERK5 deficiency suppresses tumor growth by blocking protumor macrophage polarization via STAT3 inhibition. Proc Natl Acad Sci U S A. 2018 03 20; 115(12):E2801-E2810.
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Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nat Chem Biol. 2018 04; 14(4):405-412.
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BTKCys481Ser drives ibrutinib resistance via ERK1/2 and protects BTKwild-type MYD88-mutated cells by a paracrine mechanism. Blood. 2018 05 03; 131(18):2047-2059.
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ERK5 is activated by oncogenic BRAF and promotes melanoma growth. Oncogene. 2018 05; 37(19):2601-2614.
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SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform. Cell Chem Biol. 2018 04 19; 25(4):460-470.e6.
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Allele-Specific Chromatin Recruitment and Therapeutic Vulnerabilities of ESR1 Activating Mutations. Cancer Cell. 2018 02 12; 33(2):173-186.e5.
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High MITF Expression Is Associated with Super-Enhancers and Suppressed by CDK7 Inhibition in Melanoma. J Invest Dermatol. 2018 07; 138(7):1582-1590.
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Tuning microtubule dynamics to enhance cancer therapy by modulating FER-mediated CRMP2 phosphorylation. Nat Commun. 2018 02 02; 9(1):476.
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EWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma. Cancer Cell. 2018 02 12; 33(2):202-216.e6.
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Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors. Cell Chem Biol. 2018 02 15; 25(2):135-142.e5.
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ER Stress Signaling Promotes the Survival of Cancer "Persister Cells" Tolerant to EGFR Tyrosine Kinase Inhibitors. Cancer Res. 2018 02 15; 78(4):1044-1057.
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Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nat Chem Biol. 2018 02; 14(2):163-170.
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YY1 Is a Structural Regulator of Enhancer-Promoter Loops. Cell. 2017 Dec 14; 171(7):1573-1588.e28.
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Crystal structure of human IRAK1. Proc Natl Acad Sci U S A. 2017 12 19; 114(51):13507-13512.
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A Next Generation Connectivity Map: L1000 Platform and the First 1,000,000 Profiles. Cell. 2017 Nov 30; 171(6):1437-1452.e17.
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The Library of Integrated Network-Based Cellular Signatures NIH Program: System-Level Cataloging of Human Cells Response to Perturbations. Cell Syst. 2018 01 24; 6(1):13-24.
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A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader. Cell Chem Biol. 2018 01 18; 25(1):88-99.e6.
View in: PubMed

CDK4/6 Inhibition Augments Antitumor Immunity by Enhancing T-cell Activation. Cancer Discov. 2018 02; 8(2):216-233.
View in: PubMed

Suppression of Adaptive Responses to Targeted Cancer Therapy by Transcriptional Repression. Cancer Discov. 2018 01; 8(1):59-73.
View in: PubMed

Activation of the p53 Transcriptional Program Sensitizes Cancer Cells to Cdk7 Inhibitors. Cell Rep. 2017 Oct 10; 21(2):467-481.
View in: PubMed

Enhancer profiling identifies critical cancer genes and characterizes cell identity in adult T-cell leukemia. Blood. 2017 11 23; 130(21):2326-2338.
View in: PubMed

Inhibition of USP10 induces degradation of oncogenic FLT3. Nat Chem Biol. 2017 Dec; 13(12):1207-1215.
View in: PubMed

MELK is not necessary for the proliferation of basal-like breast cancer cells. Elife. 2017 09 19; 6.
View in: PubMed

Vomocytosis of live pathogens from macrophages is regulated by the atypical MAP kinase ERK5. Sci Adv. 2017 08; 3(8):e1700898.
View in: PubMed

Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells. Nat Chem Biol. 2017 Oct; 13(10):1102-1108.
View in: PubMed

Characterization of a highly selective inhibitor of the Aurora kinases. Bioorg Med Chem Lett. 2017 09 15; 27(18):4405-4408.
View in: PubMed

Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C. Cell Chem Biol. 2017 Aug 17; 24(8):1005-1016.e3.
View in: PubMed

KRAS G12C Drug Development: Discrimination between Switch II Pocket Configurations Using Hydrogen/Deuterium-Exchange Mass Spectrometry. Structure. 2017 09 05; 25(9):1442-1448.e3.
View in: PubMed

Progress towards a public chemogenomic set for protein kinases and a call for contributions. PLoS One. 2017; 12(8):e0181585.
View in: PubMed

Gemcitabine and Chk1 Inhibitor AZD7762 Synergistically Suppress the Growth of Lkb1-Deficient Lung Adenocarcinoma. Cancer Res. 2017 09 15; 77(18):5068-5076.
View in: PubMed

Dual inhibition of Fes and Flt3 tyrosine kinases potently inhibits Flt3-ITD+ AML cell growth. PLoS One. 2017; 12(7):e0181178.
View in: PubMed

BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment. Mol Cell. 2017 Jul 06; 67(1):5-18.e19.
View in: PubMed

A UV-Independent Topical Small-Molecule Approach for Melanin Production in Human Skin. Cell Rep. 2017 06 13; 19(11):2177-2184.
View in: PubMed

Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors. Eur J Med Chem. 2017 Sep 08; 137:545-557.
View in: PubMed

The mechanism of activation of IRAK1 and IRAK4 by interleukin-1 and Toll-like receptor agonists. Biochem J. 2017 06 06; 474(12):2027-2038.
View in: PubMed

A brain-penetrant RAF dimer antagonist for the noncanonical BRAF oncoprotein of pediatric low-grade astrocytomas. Neuro Oncol. 2017 06 01; 19(6):774-785.
View in: PubMed

Synergistic interactions with PI3K inhibition that induce apoptosis. Elife. 2017 05 31; 6.
View in: PubMed

A Simple Method to Identify Kinases That Regulate Embryonic Stem Cell Pluripotency by High-throughput Inhibitor Screening. J Vis Exp. 2017 05 12; (123).
View in: PubMed

Inhibiting the oncogenic translation program is an effective therapeutic strategy in multiple myeloma. Sci Transl Med. 2017 05 10; 9(389).
View in: PubMed

Discovery of a potent dual ALK and EGFR T790M inhibitor. Eur J Med Chem. 2017 Aug 18; 136:497-510.
View in: PubMed

Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model. Sci Rep. 2017 03 28; 7(1):466.
View in: PubMed

Discoidin domain receptor 2 mediates collagen-induced activation of membrane-type 1 matrix metalloproteinase in human fibroblasts. J Biol Chem. 2017 04 21; 292(16):6633-6643.
View in: PubMed

Corrigendum: SIKs control osteocyte responses to parathyroid hormone. Nat Commun. 2017 02 22; 8:14745.
View in: PubMed

Corrigendum: THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors. Nat Commun. 2017 02 20; 8:14747.
View in: PubMed

Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent. ACS Med Chem Lett. 2017 Mar 09; 8(3):344-349.
View in: PubMed

THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors. Nat Commun. 2017 01 30; 8:14290.
View in: PubMed

Small-Molecule Inhibitors of LRRK2. Adv Neurobiol. 2017; 14:241-264.
View in: PubMed

Discovery of host-targeted covalent inhibitors of dengue virus. Antiviral Res. 2017 Mar; 139:171-179.
View in: PubMed

c-Jun N-terminal kinase promotes stem cell phenotype in triple-negative breast cancer through upregulation of Notch1 via activation of c-Jun. Oncogene. 2017 05 04; 36(18):2599-2608.
View in: PubMed

Structure-guided development of covalent TAK1 inhibitors. Bioorg Med Chem. 2017 02 01; 25(3):838-846.
View in: PubMed

Identification of compounds with anti-human cytomegalovirus activity that inhibit production of IE2 proteins. Antiviral Res. 2017 02; 138:61-67.
View in: PubMed

Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors. Bioorg Med Chem. 2017 02 15; 25(4):1320-1328.
View in: PubMed

Leveraging Gas-Phase Fragmentation Pathways for Improved Identification and Selective Detection of Targets Modified by Covalent Probes. Anal Chem. 2016 12 20; 88(24):12248-12254.
View in: PubMed

Covalent Guanosine Mimetic Inhibitors of G12C KRAS. ACS Med Chem Lett. 2017 Jan 12; 8(1):61-66.
View in: PubMed

Inactivation of KLF4 promotes T-cell acute lymphoblastic leukemia and activates the MAP2K7 pathway. Leukemia. 2017 06; 31(6):1314-1324.
View in: PubMed

A benzo[b]thiophene-based selective type 4 S1P receptor agonist. Bioorg Med Chem Lett. 2017 01 01; 27(1):1-5.
View in: PubMed

Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation. Oncotarget. 2016 Oct 25; 7(43):69760-69769.
View in: PubMed

SIKs control osteocyte responses to parathyroid hormone. Nat Commun. 2016 10 19; 7:13176.
View in: PubMed

Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors. Nat Chem Biol. 2016 10; 12(10):876-84.
View in: PubMed

Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration. Sci Transl Med. 2016 08 17; 8(352):352ra108.
View in: PubMed

Mitotic MELK-eIF4B signaling controls protein synthesis and tumor cell survival. Proc Natl Acad Sci U S A. 2016 08 30; 113(35):9810-5.
View in: PubMed

Erk5 Is a Key Regulator of Naive-Primed Transition and Embryonic Stem Cell Identity. Cell Rep. 2016 08 16; 16(7):1820-8.
View in: PubMed

Discovery of a Series of 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-ones as Selective PI3K-d/? Inhibitors. ACS Med Chem Lett. 2016 Oct 13; 7(10):908-912.
View in: PubMed

Salt-Inducible Kinase 2 Couples Ovarian Cancer Cell Metabolism with Survival at the Adipocyte-Rich Metastatic Niche. Cancer Cell. 2016 08 08; 30(2):273-289.
View in: PubMed

Corrigendum: A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nat Chem Biol. 2016 07 19; 12(8):656.
View in: PubMed

A Landscape of Pharmacogenomic Interactions in Cancer. Cell. 2016 Jul 28; 166(3):740-754.
View in: PubMed

Identification of Existing Drugs That Effectively Target NTRK1 and ROS1 Rearrangements in Lung Cancer. Clin Cancer Res. 2017 Jan 01; 23(1):204-213.
View in: PubMed

Covalent Targeting of Fibroblast Growth Factor Receptor Inhibits Metastatic Breast Cancer. . 2016 09; 15(9):2096-106.
View in: PubMed

Activation of HIPK2 Promotes ER Stress-Mediated Neurodegeneration in Amyotrophic Lateral Sclerosis. Neuron. 2016 07 06; 91(1):41-55.
View in: PubMed

Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo. ACS Chem Biol. 2016 08 19; 11(8):2105-11.
View in: PubMed

Pathophysiological significance and therapeutic targeting of germinal center kinase in diffuse large B-cell lymphoma. Blood. 2016 07 14; 128(2):239-48.
View in: PubMed

HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib. Blood. 2016 06 23; 127(25):3237-52.
View in: PubMed

Torin2 Suppresses Ionizing Radiation-Induced DNA Damage Repair. Radiat Res. 2016 05; 185(5):527-38.
View in: PubMed

A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nat Chem Biol. 2016 06; 12(6):452-8.
View in: PubMed

Discovery of a Highly Selective STK16 Kinase Inhibitor. ACS Chem Biol. 2016 06 17; 11(6):1537-43.
View in: PubMed

GNF-2 Inhibits Dengue Virus by Targeting Abl Kinases and the Viral E Protein. Cell Chem Biol. 2016 04 21; 23(4):443-52.
View in: PubMed

Targeting Myddosome Assembly in Waldenstrom Macroglobulinaemia. Br J Haematol. 2017 06; 177(5):808-813.
View in: PubMed

Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor. ACS Med Chem Lett. 2016 May 12; 7(5):476-81.
View in: PubMed

Inhibition of IKKa by BAY61-3606 Reveals IKKa-Dependent Histone H3 Phosphorylation in Human Cytomegalovirus Infected Cells. PLoS One. 2016; 11(3):e0150339.
View in: PubMed

Progress on Covalent Inhibition of KRAS(G12C). Cancer Discov. 2016 Mar; 6(3):233-4.
View in: PubMed

Inhibiting fungal multidrug resistance by disrupting an activator-Mediator interaction. Nature. 2016 Feb 25; 530(7591):485-9.
View in: PubMed

NVP-TAE684 reverses multidrug resistance (MDR) in human osteosarcoma by inhibiting P-glycoprotein (PGP1) function. Br J Pharmacol. 2016 Feb; 173(3):613-26.
View in: PubMed

EPHA2 Blockade Overcomes Acquired Resistance to EGFR Kinase Inhibitors in Lung Cancer. Cancer Res. 2016 Jan 15; 76(2):305-18.
View in: PubMed

Sustained Akt Activity Is Required to Maintain Cell Viability in Seborrheic Keratosis, a Benign Epithelial Tumor. J Invest Dermatol. 2016 Mar; 136(3):696-705.
View in: PubMed

Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis. Cancer Res. 2016 Jan 01; 76(1):127-38.
View in: PubMed

ALK inhibitor resistance in ALK(F1174L)-driven neuroblastoma is associated with AXL activation and induction of EMT. Oncogene. 2016 07 14; 35(28):3681-91.
View in: PubMed

Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. J Med Chem. 2015 Dec 10; 58(23):9296-9308.
View in: PubMed

Corrigendum: The promise and peril of chemical probes. Nat Chem Biol. 2015 Nov; 11(11):887.
View in: PubMed

The ins and outs of selective kinase inhibitor development. Nat Chem Biol. 2015 Nov; 11(11):818-21.
View in: PubMed

Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells. Oncotarget. 2015 Oct 13; 6(31):31313-22.
View in: PubMed

YAP Drives Growth by Controlling Transcriptional Pause Release from Dynamic Enhancers. Mol Cell. 2015 Oct 15; 60(2):328-37.
View in: PubMed

Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer. ACS Chem Biol. 2015 Dec 18; 10(12):2687-96.
View in: PubMed

CDK7-dependent transcriptional addiction in triple-negative breast cancer. Cell. 2015 Sep 24; 163(1):174-86.
View in: PubMed

Extracellular signal-regulated kinase 5 promotes acute cellular and systemic inflammation. Sci Signal. 2015 Aug 25; 8(391):ra86.
View in: PubMed

Development of Selective Covalent Janus Kinase 3 Inhibitors. J Med Chem. 2015 Aug 27; 58(16):6589-606.
View in: PubMed

The promise and peril of chemical probes. Nat Chem Biol. 2015 Aug; 11(8):536-41.
View in: PubMed

Discovery of a BTK/MNK dual inhibitor for lymphoma and leukemia. Leukemia. 2016 Jan; 30(1):173-81.
View in: PubMed

Hematopoietic androgen receptor deficiency promotes visceral fat deposition in male mice without impairing glucose homeostasis. Andrology. 2015 Jul; 3(4):787-96.
View in: PubMed

Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase. PLoS One. 2015; 10(6):e0128364.
View in: PubMed

Combined EGFR/MEK Inhibition Prevents the Emergence of Resistance in EGFR-Mutant Lung Cancer. Cancer Discov. 2015 Sep; 5(9):960-971.
View in: PubMed

SnapShot: Kinase Inhibitors I. Mol Cell. 2015 May 21; 58(4):708.e1.
View in: PubMed

SnapShot: Kinase Inhibitors II. Mol Cell. 2015 May 21; 58(4):710.e1.
View in: PubMed

Development of small molecules targeting the pseudokinase Her3. Bioorg Med Chem Lett. 2015 Aug 15; 25(16):3382-9.
View in: PubMed

EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors. Clin Cancer Res. 2015 Sep 01; 21(17):3913-23.
View in: PubMed

Suppression of interferon ß gene transcription by inhibitors of bromodomain and extra-terminal (BET) family members. Biochem J. 2015 Jun 15; 468(3):363-72.
View in: PubMed

Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2015 May 14; 6(5):584-9.
View in: PubMed

Identification of novel therapeutic targets in acute leukemias with NRAS mutations using a pharmacologic approach. Blood. 2015 May 14; 125(20):3133-43.
View in: PubMed

Systematic analysis of BRAF(V600E) melanomas reveals a role for JNK/c-Jun pathway in adaptive resistance to drug-induced apoptosis. Mol Syst Biol. 2015 Mar 26; 11(3):797.
View in: PubMed

EPHA2 is a mediator of vemurafenib resistance and a novel therapeutic target in melanoma. Cancer Discov. 2015 Mar; 5(3):274-87.
View in: PubMed

Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor. Cancer Cell. 2014 Dec 08; 26(6):909-922.
View in: PubMed

A Discovery Strategy for Selective Inhibitors of c-Src in Complex with the Focal Adhesion Kinase SH3/SH2-binding Region. Chem Biol Drug Des. 2015 Aug; 86(2):144-55.
View in: PubMed

CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer. Cell. 2014 Nov 20; 159(5):1126-1139.
View in: PubMed

The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma. Sci Signal. 2014 Oct 28; 7(349):ra102.
View in: PubMed

DFG-out mode of inhibition by an irreversible type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors. ACS Chem Biol. 2015 Jan 16; 10(1):299-309.
View in: PubMed

Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci U S A. 2014 Nov 11; 111(45):E4869-77.
View in: PubMed

Pharmacological targeting of the pseudokinase Her3. Nat Chem Biol. 2014 Dec; 10(12):1006-12.
View in: PubMed

Protein kinase IKKß-catalyzed phosphorylation of IRF5 at Ser462 induces its dimerization and nuclear translocation in myeloid cells. Proc Natl Acad Sci U S A. 2014 Dec 09; 111(49):17432-7.
View in: PubMed

Response and acquired resistance to everolimus in anaplastic thyroid cancer. N Engl J Med. 2014 Oct 09; 371(15):1426-33.
View in: PubMed

Systematic Identification of Culture Conditions for Induction and Maintenance of Naive Human Pluripotency. Cell Stem Cell. 2014 Oct 02; 15(4):524-526.
View in: PubMed

Molecular rationale for the use of PI3K/AKT/mTOR pathway inhibitors in combination with crizotinib in ALK-mutated neuroblastoma. Oncotarget. 2014 Sep 30; 5(18):8737-49.
View in: PubMed

A-770041 reverses paclitaxel and doxorubicin resistance in osteosarcoma cells. BMC Cancer. 2014 Sep 19; 14:681.
View in: PubMed

A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics. Nat Chem Biol. 2014 Oct; 10(10):853-60.
View in: PubMed

Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R. Clin Cancer Res. 2014 Nov 01; 20(21):5483-95.
View in: PubMed

The mitogen-activated protein kinase ERK5 regulates the development and growth of hepatocellular carcinoma. Gut. 2015 Sep; 64(9):1454-65.
View in: PubMed

Tivantinib (ARQ 197) efficacy is independent of MET inhibition in non-small-cell lung cancer cell lines. Mol Oncol. 2015 Jan; 9(1):260-9.
View in: PubMed

Screening of DUB activity and specificity by MALDI-TOF mass spectrometry. Nat Commun. 2014 Aug 27; 5:4763.
View in: PubMed

Systematic Identification of Culture Conditions for Induction and Maintenance of Naive Human Pluripotency. Cell Stem Cell. 2014 Oct 02; 15(4):523.
View in: PubMed

Small-molecule screening identifies inhibition of salt-inducible kinases as a therapeutic strategy to enhance immunoregulatory functions of dendritic cells. Proc Natl Acad Sci U S A. 2014 Aug 26; 111(34):12468-73.
View in: PubMed

Chemical interrogation of the malaria kinome. Chembiochem. 2014 Sep 05; 15(13):1920-30.
View in: PubMed

The LKB1-salt-inducible kinase pathway functions as a key gluconeogenic suppressor in the liver. Nat Commun. 2014 Aug 04; 5:4535.
View in: PubMed

Discovery of type II inhibitors of TGFß-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J Med Chem. 2015 Jan 08; 58(1):183-96.
View in: PubMed

Systematic identification of culture conditions for induction and maintenance of naive human pluripotency. Cell Stem Cell. 2014 10 02; 15(4):471-487.
View in: PubMed

Time from first presentation in primary care to treatment of symptomatic colorectal cancer: effect on disease stage and survival. Br J Cancer. 2014 Jul 29; 111(3):461-9.
View in: PubMed

Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31; 511(7511):616-20.
View in: PubMed

Ligand-associated ERBB2/3 activation confers acquired resistance to FGFR inhibition in FGFR3-dependent cancer cells. Oncogene. 2015 Apr 23; 34(17):2167-77.
View in: PubMed

In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C. Proc Natl Acad Sci U S A. 2014 Jun 17; 111(24):8895-900.
View in: PubMed

MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells. Elife. 2014 May 20; 3:e01763.
View in: PubMed

Fluorescent visualization of Src by using dasatinib-BODIPY. Chembiochem. 2014 Jun 16; 15(9):1317-24.
View in: PubMed

Identification of Wee1 as a novel therapeutic target for mutant RAS-driven acute leukemia and other malignancies. Leukemia. 2015 Jan; 29(1):27-37.
View in: PubMed

Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery? ACS Chem Biol. 2014 Jun 20; 9(6):1230-41.
View in: PubMed

Structural mechanisms determining inhibition of the collagen receptor DDR1 by selective and multi-targeted type II kinase inhibitors. J Mol Biol. 2014 Jun 26; 426(13):2457-70.
View in: PubMed

Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC. J Clin Invest. 2014 May; 124(5):2037-49.
View in: PubMed

Interleukin-6 secretion by astrocytes is dynamically regulated by PI3K-mTOR-calcium signaling. PLoS One. 2014; 9(3):e92649.
View in: PubMed

PIM kinases are essential for chronic lymphocytic leukemia cell survival (PIM2/3) and CXCR4-mediated microenvironmental interactions (PIM1). . 2014 May; 13(5):1231-45.
View in: PubMed

Discovery of a potent, covalent BTK inhibitor for B-cell lymphoma. ACS Chem Biol. 2014 May 16; 9(5):1086-91.
View in: PubMed

Correction to Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor. ACS Chem Biol. 2014 Mar 21; 9(3):840.
View in: PubMed

Protected amine labels: a versatile molecular scaffold for multiplexed nominal mass and sub-Da isotopologue quantitative proteomic reagents. J Am Soc Mass Spectrom. 2014 Apr; 25(4):636-50.
View in: PubMed

Discovery of allosteric BCR-ABL inhibitors from phenotypic screen to clinical candidate. Methods Enzymol. 2014; 548:173-88.
View in: PubMed

Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 01; 457(1):215-25.
View in: PubMed

Acquired resistance to dasatinib in lung cancer cell lines conferred by DDR2 gatekeeper mutation and NF1 loss. . 2014 Feb; 13(2):475-82.
View in: PubMed

Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor. Angew Chem Int Ed Engl. 2014 Jan 03; 53(1):199-204.
View in: PubMed

Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem. 2013; 70:758-67.
View in: PubMed

Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells. . 2013 Dec; 12(12):2651-62.
View in: PubMed

Digital pattern recognition-based image analysis quantifies immune infiltrates in distinct tissue regions of colorectal cancer and identifies a metastatic phenotype. Br J Cancer. 2013 Sep 17; 109(6):1618-24.
View in: PubMed

Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18; 8(10):2145-50.
View in: PubMed

Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs. J Natl Cancer Inst. 2013 Sep 04; 105(17):1322-31.
View in: PubMed

mTORC1 phosphorylation sites encode their sensitivity to starvation and rapamycin. Science. 2013 Jul 26; 341(6144):1236566.
View in: PubMed

A mutation in MYD88 (L265P) supports the survival of lymphoplasmacytic cells by activation of Bruton tyrosine kinase in Waldenström macroglobulinemia. Blood. 2013 Aug 15; 122(7):1222-32.
View in: PubMed

Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells. Nat Biotechnol. 2013 Jul; 31(7):630-7.
View in: PubMed

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 clinical trials. J Med Chem. 2013 Jul 25; 56(14):5675-90.
View in: PubMed

Inhibitor-sensitive FGFR2 and FGFR3 mutations in lung squamous cell carcinoma. Cancer Res. 2013 Aug 15; 73(16):5195-205.
View in: PubMed

Metabolic and functional genomic studies identify deoxythymidylate kinase as a target in LKB1-mutant lung cancer. Cancer Discov. 2013 Aug; 3(8):870-9.
View in: PubMed

X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. J Med Chem. 2013 Jun 13; 56(11):4413-21.
View in: PubMed

Discovery of a selective irreversible BMX inhibitor for prostate cancer. ACS Chem Biol. 2013 Jul 19; 8(7):1423-8.
View in: PubMed

TSC1 involvement in bladder cancer: diverse effects and therapeutic implications. J Pathol. 2013 May; 230(1):17-27.
View in: PubMed

Pharmacological inhibition of Eph receptors enhances glucose-stimulated insulin secretion from mouse and human pancreatic islets. Diabetologia. 2013 Jun; 56(6):1350-5.
View in: PubMed

TYK2-STAT1-BCL2 pathway dependence in T-cell acute lymphoblastic leukemia. Cancer Discov. 2013 May; 3(5):564-77.
View in: PubMed

Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR. Cancer Res. 2013 Apr 15; 73(8):2574-86.
View in: PubMed

Selective Akt inhibitors synergize with tyrosine kinase inhibitors and effectively override stroma-associated cytoprotection of mutant FLT3-positive AML cells. PLoS One. 2013; 8(2):e56473.
View in: PubMed

Developing irreversible inhibitors of the protein kinase cysteinome. Chem Biol. 2013 Feb 21; 20(2):146-59.
View in: PubMed

Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. ACS Med Chem Lett. 2013 Mar 14; 4(3):333-7.
View in: PubMed

A public-private partnership to unlock the untargeted kinome. Nat Chem Biol. 2013 Jan; 9(1):3-6.
View in: PubMed

Resistance to irreversible EGF receptor tyrosine kinase inhibitors through a multistep mechanism involving the IGF1R pathway. Cancer Res. 2013 Jan 15; 73(2):834-43.
View in: PubMed

Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 - 2011). Expert Opin Ther Pat. 2012 Dec; 22(12):1415-26.
View in: PubMed

The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate. Br J Pharmacol. 2012 Nov; 167(5):1035-47.
View in: PubMed

Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc Natl Acad Sci U S A. 2012 Oct 16; 109(42):16986-91.
View in: PubMed

Leveraging kinase inhibitors to develop small molecule tools for imaging kinases by fluorescence microscopy. Mol Biosyst. 2012 Oct; 8(10):2523-6.
View in: PubMed

Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors. Cancer Discov. 2012 Oct; 2(10):934-47.
View in: PubMed

BMK1 is involved in the regulation of p53 through disrupting the PML-MDM2 interaction. Oncogene. 2013 Jun 27; 32(26):3156-64.
View in: PubMed

BAY61-3606 affects the viability of colon cancer cells in a genotype-directed manner. PLoS One. 2012; 7(7):e41343.
View in: PubMed

Dual blockade of lipid and cyclin-dependent kinases induces synthetic lethality in malignant glioma. Proc Natl Acad Sci U S A. 2012 Jul 31; 109(31):12722-7.
View in: PubMed

Systematic kinome shRNA screening identifies CDK11 (PITSLRE) kinase expression is critical for osteosarcoma cell growth and proliferation. Clin Cancer Res. 2012 Sep 01; 18(17):4580-8.
View in: PubMed

The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma. Cancer Cell. 2012 Jul 10; 22(1):117-30.
View in: PubMed

GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorg Med Chem Lett. 2012 Sep 01; 22(17):5625-9.
View in: PubMed

Development of 'DFG-out' inhibitors of gatekeeper mutant kinases. Bioorg Med Chem Lett. 2012 Aug 15; 22(16):5297-302.
View in: PubMed

The IkappaB kinase family phosphorylates the Parkinson's disease kinase LRRK2 at Ser935 and Ser910 during Toll-like receptor signaling. PLoS One. 2012; 7(6):e39132.
View in: PubMed

Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2012 Aug 09; 3(8):658-662.
View in: PubMed

An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFRa and kit. Bioorg Med Chem Lett. 2012 Jul 15; 22(14):4579-84.
View in: PubMed

A unifying model for mTORC1-mediated regulation of mRNA translation. Nature. 2012 May 02; 485(7396):109-13.
View in: PubMed

Small-molecule inhibitors of the c-Fes protein-tyrosine kinase. Chem Biol. 2012 Apr 20; 19(4):529-40.
View in: PubMed

Selective ATP-competitive inhibitors of TOR suppress rapamycin-insensitive function of TORC2 in Saccharomyces cerevisiae. ACS Chem Biol. 2012 Jun 15; 7(6):982-7.
View in: PubMed

Functional characterization of an isoform-selective inhibitor of PI3K-p110ß as a potential anticancer agent. Cancer Discov. 2012 May; 2(5):425-33.
View in: PubMed

Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib/multi-targeted inhibitors and JAK inhibitors. Leukemia. 2012 Oct; 26(10):2233-44.
View in: PubMed

Systematic identification of genomic markers of drug sensitivity in cancer cells. Nature. 2012 Mar 28; 483(7391):570-5.
View in: PubMed

Characterization of TAE684 as a potent LRRK2 kinase inhibitor. Bioorg Med Chem Lett. 2012 Mar 01; 22(5):1864-9.
View in: PubMed

Discovery of potent and selective covalent inhibitors of JNK. Chem Biol. 2012 Jan 27; 19(1):140-54.
View in: PubMed

Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics. J Biol Chem. 2012 Mar 23; 287(13):9742-9752.
View in: PubMed

Development of ATP-competitive mTOR inhibitors. Methods Mol Biol. 2012; 821:447-60.
View in: PubMed

Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen. ACS Chem Biol. 2012 Jan 20; 7(1):185-96.
View in: PubMed

Oncogenic PIK3CA-driven mammary tumors frequently recur via PI3K pathway-dependent and PI3K pathway-independent mechanisms. Nat Med. 2011 Aug 07; 17(9):1116-20.
View in: PubMed

High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors. Chem Biol. 2011 Jul 29; 18(7):868-79.
View in: PubMed

A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. Cancer Res. 2011 Sep 15; 71(18):6051-60.
View in: PubMed

Microenvironmental influence on pre-clinical activity of polo-like kinase inhibition in multiple myeloma: implications for clinical translation. PLoS One. 2011; 6(7):e20226.
View in: PubMed

In situ kinase profiling reveals functionally relevant properties of native kinases. Chem Biol. 2011 Jun 24; 18(6):699-710.
View in: PubMed

The mTOR-regulated phosphoproteome reveals a mechanism of mTORC1-mediated inhibition of growth factor signaling. Science. 2011 Jun 10; 332(6035):1317-22.
View in: PubMed

Inhibitor-sensitive FGFR1 amplification in human non-small cell lung cancer. PLoS One. 2011; 6(6):e20351.
View in: PubMed

Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer. Cancer Discov. 2011 Jun; 1(1):78-89.
View in: PubMed

Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability. Bioorg Med Chem Lett. 2011 Jul 01; 21(13):4036-40.
View in: PubMed

The evolving war on cancer. Cell. 2011 Apr 01; 145(1):19-24.
View in: PubMed

Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. ACS Med Chem Lett. 2011 May 12; 2(5):379-384.
View in: PubMed

Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat Chem Biol. 2011 Apr; 7(4):203-5.
View in: PubMed

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. J Med Chem. 2011 Mar 10; 54(5):1473-80.
View in: PubMed

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. ACS Med Chem Lett. 2011 Mar 10; 2(3):195-200.
View in: PubMed

Allosteric interactions between the myristate- and ATP-site of the Abl kinase. PLoS One. 2011 Jan 10; 6(1):e15929.
View in: PubMed

Small molecule modulators of antioxidant response pathway. Curr Opin Chem Biol. 2011 Feb; 15(1):162-73.
View in: PubMed

Long-term psychosocial impact of alternative management policies in women with low-grade abnormal cervical cytology referred for colposcopy: a randomised controlled trial. Br J Cancer. 2011 Jan 18; 104(2):255-64.
View in: PubMed

Discovery of selective irreversible inhibitors for EGFR-T790M. Bioorg Med Chem Lett. 2011 Jan 15; 21(2):638-43.
View in: PubMed

The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers. Cancer Res. 2010 Dec 15; 70(24):10038-43.
View in: PubMed

Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene. Cancer Res. 2010 Dec 01; 70(23):9827-36.
View in: PubMed

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. J Med Chem. 2010 Oct 14; 53(19):7146-55.
View in: PubMed

Expanding the diversity of allosteric bcr-abl inhibitors. J Med Chem. 2010 Oct 14; 53(19):6934-46.
View in: PubMed

Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell. 2010 Sep 14; 18(3):258-67.
View in: PubMed

Discovery and characterization of novel mutant FLT3 kinase inhibitors. . 2010 Sep; 9(9):2468-77.
View in: PubMed

A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl. J Med Chem. 2010 Aug 12; 53(15):5439-48.
View in: PubMed

Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials. Bioorg Med Chem Lett. 2010 Jul 15; 20(14):4027-31.
View in: PubMed

A small-molecule inducer of the antioxidant response element. Chem Biol. 2010 May 28; 17(5):537-47.
View in: PubMed

Beneficial effects of combining a type II ATP competitive inhibitor with an allosteric competitive inhibitor of BCR-ABL for the treatment of imatinib-sensitive and imatinib-resistant CML. Leukemia. 2010 Jul; 24(7):1375-8.
View in: PubMed

Broad spectrum alkynyl inhibitors of T315I Bcr-Abl. Bioorg Med Chem Lett. 2010 Jul 15; 20(14):4196-200.
View in: PubMed

Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May; 6(5):359-68.
View in: PubMed

A structure-guided approach to creating covalent FGFR inhibitors. Chem Biol. 2010 Mar 26; 17(3):285-95.
View in: PubMed

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. Blood. 2010 May 27; 115(21):4206-16.
View in: PubMed

Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site. Biochim Biophys Acta. 2010 Mar; 1804(3):454-62.
View in: PubMed

Acquired resistance of non-small cell lung cancer cells to MET kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency. Cancer Res. 2010 Feb 15; 70(4):1625-34.
View in: PubMed

Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature. 2010 Jan 28; 463(7280):501-6.
View in: PubMed

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24; 462(7276):1070-4.
View in: PubMed

MEK1 mutations confer resistance to MEK and B-RAF inhibition. Proc Natl Acad Sci U S A. 2009 Dec 01; 106(48):20411-6.
View in: PubMed

Cell-based optimization of novel benzamides as potential antimalarial leads. Bioorg Med Chem Lett. 2009 Dec 15; 19(24):6970-4.
View in: PubMed

Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II. Bioorg Med Chem Lett. 2009 Dec 01; 19(23):6691-5.
View in: PubMed

N-myristoylated c-Abl tyrosine kinase localizes to the endoplasmic reticulum upon binding to an allosteric inhibitor. J Biol Chem. 2009 Oct 16; 284(42):29005-14.
View in: PubMed

Factors underlying sensitivity of cancers to small-molecule kinase inhibitors. Nat Rev Drug Discov. 2009 Sep; 8(9):709-23.
View in: PubMed

Characterization of AZD8931, a potent reversible small molecule inhibitor against epidermal growth factor receptor (EGFR), erythroblastic leukemia viral oncogene homolog 2 (HER2) and 3 (HER3) with a unique and balanced pharmacological profile. J Clin Oncol. 2009 May 20; 27(15_suppl):11072.
View in: PubMed

FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML. Drug Resist Updat. 2009 Jun; 12(3):81-9.
View in: PubMed

DEPTOR is an mTOR inhibitor frequently overexpressed in multiple myeloma cells and required for their survival. Cell. 2009 May 29; 137(5):873-86.
View in: PubMed

Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2009 Aug 01; 19(15):4467-70.
View in: PubMed

A ceramide-1-phosphate analogue, PCERA-1, simultaneously suppresses tumour necrosis factor-alpha and induces interleukin-10 production in activated macrophages. Immunology. 2009 May; 127(1):103-15.
View in: PubMed

Fibroblast growth factor receptor 1-transformed mammary epithelial cells are dependent on RSK activity for growth and survival. Cancer Res. 2009 Mar 15; 69(6):2244-51.
View in: PubMed

Golgicide A reveals essential roles for GBF1 in Golgi assembly and function. Nat Chem Biol. 2009 Mar; 5(3):157-65.
View in: PubMed

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. Immunol Lett. 2009 Mar 24; 123(1):1-8.
View in: PubMed

Conformational disturbance in Abl kinase upon mutation and deregulation. Proc Natl Acad Sci U S A. 2009 Feb 03; 106(5):1386-91.
View in: PubMed

An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem. 2009 Mar 20; 284(12):8023-32.
View in: PubMed

mTOR Mediated Anti-Cancer Drug Discovery. Drug Discov Today Ther Strateg. 2009; 6(2):47-55.
View in: PubMed

Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer. 2009 Jan; 9(1):28-39.
View in: PubMed

Activating mutations in ALK provide a therapeutic target in neuroblastoma. Nature. 2008 Oct 16; 455(7215):975-8.
View in: PubMed

Activation of tyrosine kinases by mutation of the gatekeeper threonine. Nat Struct Mol Biol. 2008 Oct; 15(10):1109-18.
View in: PubMed

Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I. Bioorg Med Chem Lett. 2008 Oct 15; 18(20):5618-21.
View in: PubMed

Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. Bioorg Med Chem Lett. 2008 Nov 15; 18(22):5916-9.
View in: PubMed

EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer. Clin Cancer Res. 2008 Jul 01; 14(13):4275-83.
View in: PubMed

In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. Proc Natl Acad Sci U S A. 2008 Jul 01; 105(26):9059-64.
View in: PubMed

Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. Nat Chem Biol. 2008 Jun; 4(6):347-56.
View in: PubMed

Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Res. 2008 May 01; 68(9):3389-95.
View in: PubMed

High-throughput kinase profiling as a platform for drug discovery. Nat Rev Drug Discov. 2008 May; 7(5):391-7.
View in: PubMed

Discovery of selective aminothiazole aurora kinase inhibitors. ACS Chem Biol. 2008 Mar 20; 3(3):180-92.
View in: PubMed

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci U S A. 2007 Dec 11; 104(50):19936-41.
View in: PubMed

Verification of a designed intramolecular hydrogen bond in a drug scaffold by nuclear magnetic resonance spectroscopy. J Med Chem. 2007 Nov 29; 50(24):5875-7.
View in: PubMed

Chemical proteomics identifies unanticipated targets of clinical kinase inhibitors. ACS Chem Biol. 2007 Oct 19; 2(10):661-4.
View in: PubMed

Identification of human kinases involved in hepatitis C virus replication by small interference RNA library screening. J Biol Chem. 2008 Jan 04; 283(1):29-36.
View in: PubMed

Identification and characterization of small-molecule inducers of epidermal keratinocyte differentiation. ACS Chem Biol. 2007 Mar 20; 2(3):171-5.
View in: PubMed

Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proc Natl Acad Sci U S A. 2007 Jan 02; 104(1):270-5.
View in: PubMed

Drug discovery through industry-academic partnerships. Nat Chem Biol. 2006 Dec; 2(12):649-53.
View in: PubMed

A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model. Chem Biol. 2006 Nov; 13(11):1227-34.
View in: PubMed

Rational design of inhibitors that bind to inactive kinase conformations. Nat Chem Biol. 2006 Jul; 2(7):358-64.
View in: PubMed

A general strategy for creating "inactive-conformation" abl inhibitors. Chem Biol. 2006 Jul; 13(7):779-86.
View in: PubMed

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2. Bioorg Med Chem Lett. 2006 May 15; 16(10):2689-92.
View in: PubMed

Antimitotic agents of natural origin. Curr Drug Targets. 2006 Mar; 7(3):305-26.
View in: PubMed

Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. J Am Chem Soc. 2006 Feb 22; 128(7):2182-3.
View in: PubMed

An efficient rapid system for profiling the cellular activities of molecular libraries. Proc Natl Acad Sci U S A. 2006 Feb 28; 103(9):3153-8.
View in: PubMed

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1. Bioorg Med Chem Lett. 2006 Apr 15; 16(8):2173-6.
View in: PubMed

Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol. 2006 Feb; 2(2):95-102.
View in: PubMed

Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors. Bioorg Med Chem Lett. 2005 Dec 15; 15(24):5467-73.
View in: PubMed

Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives. J Biol Chem. 2005 Sep 02; 280(35):31220-9.
View in: PubMed

Roscovitine targets, protein kinases and pyridoxal kinase. J Biol Chem. 2005 Sep 02; 280(35):31208-19.
View in: PubMed

A genome-wide overexpression screen in yeast for small-molecule target identification. Chem Biol. 2005 Jan; 12(1):55-63.
View in: PubMed

Creating chemical diversity to target protein kinases. Comb Chem High Throughput Screen. 2004 Aug; 7(5):453-72.
View in: PubMed

Reducing tobacco addiction through tobacco product regulation. Tob Control. 2004 Jun; 13(2):132-5.
View in: PubMed

Small molecules that induce cardiomyogenesis in embryonic stem cells. J Am Chem Soc. 2004 Feb 18; 126(6):1590-1.
View in: PubMed

Synthesis and target identification of hymenialdisine analogs. Chem Biol. 2004 Feb; 11(2):247-59.
View in: PubMed

Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J Biol Chem. 2004 Apr 02; 279(14):13839-48.
View in: PubMed

Identification of a novel protein regulating microtubule stability through a chemical approach. Chem Biol. 2004 Jan; 11(1):135-46.
View in: PubMed

European Code Against Cancer and scientific justification: third version (2003). Ann Oncol. 2003 Jul; 14(7):973-1005.
View in: PubMed

Synthetic small molecules that control stem cell fate. Proc Natl Acad Sci U S A. 2003 Jun 24; 100(13):7632-7.
View in: PubMed

Identification of homeodomain proteins, PBX1 and PREP1, involved in the transcription of murine leukemia virus. Mol Cell Biol. 2003 Feb; 23(3):831-41.
View in: PubMed

SRC family kinases: potential targets for the treatment of human cancer and leukemia. Curr Pharm Des. 2003; 9(25):2043-59.
View in: PubMed

Optimization of experimental antimitotic agents: classical and combinatorial methods. Prog Cell Cycle Res. 2003; 5:135-43.
View in: PubMed

Chemical and biological profile of dual Cdk1 and Cdk2 inhibitors. Curr Med Chem Anticancer Agents. 2003 Jan; 3(1):1-14.
View in: PubMed

A small molecule with osteogenesis-inducing activity in multipotent mesenchymal progenitor cells. J Am Chem Soc. 2002 Dec 11; 124(49):14520-1.
View in: PubMed

p42/p44 MAPKs are intracellular targets of the CDK inhibitor purvalanol. Oncogene. 2002 Sep 19; 21(42):6413-24.
View in: PubMed

Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase. Chembiochem. 2002 Sep 02; 3(9):897-901.
View in: PubMed

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. J Virol. 2002 Aug; 76(15):7874-82.
View in: PubMed

Resin-capture and release strategy toward combinatorial libraries of 2,6,9-substituted purines. J Comb Chem. 2002 Mar-Apr; 4(2):183-6.
View in: PubMed

A combinatorial scaffold approach toward kinase-directed heterocycle libraries. J Am Chem Soc. 2002 Feb 27; 124(8):1594-6.
View in: PubMed

Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors. J Med Chem. 2001 Dec 20; 44(26):4497-500.
View in: PubMed

A concise and traceless linker strategy toward combinatorial libraries of 2,6,9-substituted purines. J Org Chem. 2001 Nov 30; 66(24):8273-6.
View in: PubMed

Solid-phase synthesis of 2,3,5-trisubstituted indoles. Org Lett. 2001 Nov 29; 3(24):3827-30.
View in: PubMed

Design of allele-specific protein methyltransferase inhibitors. J Am Chem Soc. 2001 Nov 28; 123(47):11608-13.
View in: PubMed

Combinatorial libraries and biological discovery. Curr Opin Neurobiol. 2001 Oct; 11(5):608-14.
View in: PubMed

Discovery of estrogen sulfotransferase inhibitors from a purine library screen. J Med Chem. 2001 Aug 16; 44(17):2683-6.
View in: PubMed

Structure-activity relationships and inhibitory effects of various purine derivatives on the in vitro growth of Plasmodium falciparum. Biochem Pharmacol. 2001 Aug 01; 62(3):341-8.
View in: PubMed

The establishment of human research tissue banking in the UK and several western European countries. The report and recommendations of ECVAM Workshop 44. Altern Lab Anim. 2001 Mar-Apr; 29(2):125-34.
View in: PubMed

A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature. 2000 Sep 21; 407(6802):395-401.
View in: PubMed

Intracellular targets of cyclin-dependent kinase inhibitors: identification by affinity chromatography using immobilised inhibitors. Chem Biol. 2000 Jun; 7(6):411-22.
View in: PubMed

ATP-site directed inhibitors of cyclin-dependent kinases. Curr Med Chem. 1999 Sep; 6(9):859-75.
View in: PubMed

Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors. Chem Biol. 1999 Jun; 6(6):361-75.
View in: PubMed

A cyclin-dependent kinase inhibitor inducing cancer cell differentiation: biochemical identification using Xenopus egg extracts. Proc Natl Acad Sci U S A. 1999 Apr 27; 96(9):4797-802.
View in: PubMed

Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul 24; 281(5376):533-8.
View in: PubMed

CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation. J Biol Chem. 1997 Nov 14; 272(46):29207-11.
View in: PubMed

Informed consent. British institutions collaborating in projects overseas may face dilemma. BMJ. 1997 Jul 26; 315(7102):248.
View in: PubMed

Prevention and early detection of lung cancer-clinical aspects. Lung Cancer. 1997 May; 17(1):163-74.
View in: PubMed

Effects of nicotine and amphetamine on latent inhibition in human subjects. Psychopharmacology (Berl). 1996 Sep; 127(2):164-73.
View in: PubMed

The immunological evolution of catalysis. Science. 1996 Feb 23; 271(5252):1086-91.
View in: PubMed

Prevalence of obesity in American Indians and Alaska Natives. Am J Clin Nutr. 1991 06; 53(6 Suppl):1535S-1542S.
View in: PubMed

A review of the in vitro and in vivo neurochemical characterization of the NMDA/PCP/glycine/ion channel receptor macrocomplex. Neurochem Res. 1990 Feb; 15(2):217-30.
View in: PubMed

The etiology of adolescents' perceptions of their weight. J Youth Adolesc. 1986 Dec; 15(6):461-74.
View in: PubMed

Effect of Sabin Type 1 poliomyelitis vaccine administered by mouth to newborn infants. N Engl J Med. 1961 May 25; 264:1071-8.
View in: PubMed

Studies on an attenuated measles-virus vaccine. V. Clinical, antigenic and prophylactic effects of vaccine in institutionalized and home-dwelling children. N Engl J Med. 1960 Jul 28; 263:170-3.
View in: PubMed

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