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Item TypeName
Academic Article p42/p44 MAPKs are intracellular targets of the CDK inhibitor purvalanol.
Academic Article Intracellular targets of cyclin-dependent kinase inhibitors: identification by affinity chromatography using immobilised inhibitors.
Academic Article Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase.
Academic Article Allosteric inhibitors of Bcr-abl-dependent cell proliferation.
Academic Article A combinatorial scaffold approach toward kinase-directed heterocycle libraries.
Academic Article Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors.
Academic Article Expanding the diversity of allosteric bcr-abl inhibitors.
Academic Article Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
Academic Article Chemical and biological profile of dual Cdk1 and Cdk2 inhibitors.
Academic Article Discovery of selective aminothiazole aurora kinase inhibitors.
Academic Article Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.
Academic Article Inhibitor-sensitive FGFR1 amplification in human non-small cell lung cancer.
Academic Article Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors.
Academic Article Activation of tyrosine kinases by mutation of the gatekeeper threonine.
Academic Article High-throughput kinase profiling as a platform for drug discovery.
Academic Article Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.
Academic Article 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.
Academic Article Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility.
Academic Article Development of 'DFG-out' inhibitors of gatekeeper mutant kinases.
Academic Article A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl.
Academic Article Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors.
Academic Article MEK1 mutations confer resistance to MEK and B-RAF inhibition.
Academic Article Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.
Academic Article Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors.
Academic Article GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.
Academic Article High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors.
Academic Article Development of ATP-competitive mTOR inhibitors.
Academic Article Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics.
Academic Article Acquired resistance of non-small cell lung cancer cells to MET kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency.
Academic Article A structure-guided approach to creating covalent FGFR inhibitors.
Academic Article Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library.
Academic Article Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.
Academic Article Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors.
Academic Article EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer.
Academic Article Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site.
Academic Article The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers.
Academic Article Selective ATP-competitive inhibitors of TOR suppress rapamycin-insensitive function of TORC2 in Saccharomyces cerevisiae.
Academic Article A cyclin-dependent kinase inhibitor inducing cancer cell differentiation: biochemical identification using Xenopus egg extracts.
Academic Article Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives.
Academic Article An efficient rapid system for profiling the cellular activities of molecular libraries.
Academic Article Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.
Academic Article A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors.
Academic Article A genome-wide overexpression screen in yeast for small-molecule target identification.
Academic Article Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1.
Academic Article The IkappaB kinase family phosphorylates the Parkinson's disease kinase LRRK2 at Ser935 and Ser910 during Toll-like receptor signaling.
Academic Article Resistance to irreversible EGF receptor tyrosine kinase inhibitors through a multistep mechanism involving the IGF1R pathway.
Academic Article 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.
Academic Article Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.
Academic Article Small-molecule inhibitors of the c-Fes protein-tyrosine kinase.
Academic Article 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.
Academic Article Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene.
Academic Article Selective Akt inhibitors synergize with tyrosine kinase inhibitors and effectively override stroma-associated cytoprotection of mutant FLT3-positive AML cells.
Academic Article Creating chemical diversity to target protein kinases.
Academic Article TSC1 involvement in bladder cancer: diverse effects and therapeutic implications.
Academic Article CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation.
Academic Article Roscovitine targets, protein kinases and pyridoxal kinase.
Academic Article Factors underlying sensitivity of cancers to small-molecule kinase inhibitors.
Academic Article Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.
Academic Article N-myristoylated c-Abl tyrosine kinase localizes to the endoplasmic reticulum upon binding to an allosteric inhibitor.
Academic Article In situ kinase profiling reveals functionally relevant properties of native kinases.
Academic Article Identification of human kinases involved in hepatitis C virus replication by small interference RNA library screening.
Academic Article Rational design of inhibitors that bind to inactive kinase conformations.
Academic Article FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML.
Academic Article Microenvironmental influence on pre-clinical activity of polo-like kinase inhibition in multiple myeloma: implications for clinical translation.
Academic Article The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma.
Academic Article Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.
Academic Article Discovery of selective irreversible inhibitors for EGFR-T790M.
Academic Article Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen.
Academic Article Activating mutations in ALK provide a therapeutic target in neuroblastoma.
Academic Article Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors.
Academic Article Functional characterization of an isoform-selective inhibitor of PI3K-p110ß as a potential anticancer agent.
Academic Article Targeting cancer with small molecule kinase inhibitors.
Academic Article Conformational disturbance in Abl kinase upon mutation and deregulation.
Academic Article Systematic kinome shRNA screening identifies CDK11 (PITSLRE) kinase expression is critical for osteosarcoma cell growth and proliferation.
Academic Article Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib/multi-targeted inhibitors and JAK inhibitors.
Academic Article Dual blockade of lipid and cyclin-dependent kinases induces synthetic lethality in malignant glioma.
Academic Article 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.
Academic Article Discovery of potent and selective covalent inhibitors of JNK.
Academic Article Leveraging kinase inhibitors to develop small molecule tools for imaging kinases by fluorescence microscopy.
Academic Article Developing irreversible inhibitors of the protein kinase cysteinome.
Academic Article Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2.
Academic Article Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 - 2011).
Academic Article TYK2-STAT1-BCL2 pathway dependence in T-cell acute lymphoblastic leukemia.
Academic Article A chemical switch for inhibitor-sensitive alleles of any protein kinase.
Academic Article Chemical proteomics identifies unanticipated targets of clinical kinase inhibitors.
Academic Article Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Academic Article Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.
Academic Article An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFRa and kit.
Academic Article Discovery and characterization of novel mutant FLT3 kinase inhibitors.
Academic Article Allosteric interactions between the myristate- and ATP-site of the Abl kinase.
Academic Article Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer.
Concept MAP Kinase Kinase 4
Concept Mitogen-Activated Protein Kinase 3
Concept Class Ia Phosphatidylinositol 3-Kinase
Concept Cyclin-Dependent Kinase 5
Concept MAP Kinase Kinase 7
Concept Mitogen-Activated Protein Kinase Kinases
Concept Janus Kinase 3
Concept MAP Kinase Kinase Kinases
Concept Mitogen-Activated Protein Kinase 7
Concept Phosphatidylinositol 3-Kinase
Concept Cyclin-Dependent Kinase 2
Concept Protein Kinase Inhibitors
Concept Cyclin-Dependent Kinase Inhibitor p21
Concept Mitogen-Activated Protein Kinase 1
Concept Mitogen-Activated Protein Kinase 9
Concept CDC2 Protein Kinase
Concept Janus Kinase 1
Concept TYK2 Kinase
Concept MAP Kinase Kinase 2
Concept Mitogen-Activated Protein Kinase 8
Concept Nucleoside-Phosphate Kinase
Concept I-kappa B Kinase
Concept Cyclin-Dependent Kinase 8
Concept Cyclin-Dependent Kinase 6
Concept Focal Adhesion Kinase 1
Concept Cyclin-Dependent Kinase 9
Concept CDC28 Protein Kinase, S cerevisiae
Concept Cyclin-Dependent Kinase 4
Concept MAP Kinase Signaling System
Concept Protein Kinase C
Concept MAP Kinase Kinase 5
Concept Lymphocyte Specific Protein Tyrosine Kinase p56(lck)
Concept MAP Kinase Kinase 1
Concept fms-Like Tyrosine Kinase 3
Concept MAP Kinase Kinase Kinase 1
Concept Pyridoxal Kinase
Academic Article Metabolic and functional genomic studies identify deoxythymidylate kinase as a target in LKB1-mutant lung cancer.
Academic Article Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells.
Academic Article Inhibitor-sensitive FGFR2 and FGFR3 mutations in lung squamous cell carcinoma.
Academic Article A mutation in MYD88 (L265P) supports the survival of lymphoplasmacytic cells by activation of Bruton tyrosine kinase in Waldenström macroglobulinemia.
Academic Article Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR.
Academic Article Pharmacological inhibition of Eph receptors enhances glucose-stimulated insulin secretion from mouse and human pancreatic islets.
Academic Article Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor.
Academic Article X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor.
Academic Article BMK1 is involved in the regulation of p53 through disrupting the PML-MDM2 interaction.
Academic Article Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones.
Academic Article Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases.
Academic Article 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.
Academic Article Discovery of a selective irreversible BMX inhibitor for prostate cancer.
Academic Article Correction to Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor.
Academic Article Acquired resistance to dasatinib in lung cancer cell lines conferred by DDR2 gatekeeper mutation and NF1 loss.
Academic Article Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC.
Academic Article PIM kinases are essential for chronic lymphocytic leukemia cell survival (PIM2/3) and CXCR4-mediated microenvironmental interactions (PIM1).
Academic Article Discovery of a potent, covalent BTK inhibitor for B-cell lymphoma.
Academic Article Structural mechanisms determining inhibition of the collagen receptor DDR1 by selective and multi-targeted type II kinase inhibitors.
Academic Article Fluorescent visualization of Src by using dasatinib-BODIPY.
Academic Article MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells.
Academic Article Chemical interrogation of the malaria kinome.
Academic Article Small-molecule screening identifies inhibition of salt-inducible kinases as a therapeutic strategy to enhance immunoregulatory functions of dendritic cells.
Academic Article The LKB1-salt-inducible kinase pathway functions as a key gluconeogenic suppressor in the liver.
Academic Article Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery?
Academic Article A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics.
Academic Article Discovery of type II inhibitors of TGFß-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2).
Academic Article A-770041 reverses paclitaxel and doxorubicin resistance in osteosarcoma cells.
Academic Article Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R.
Academic Article The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma.
Academic Article Molecular rationale for the use of PI3K/AKT/mTOR pathway inhibitors in combination with crizotinib in ALK-mutated neuroblastoma.
Academic Article Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.
Academic Article Pharmacological targeting of the pseudokinase Her3.
Academic Article Discovery of allosteric BCR-ABL inhibitors from phenotypic screen to clinical candidate.
Academic Article CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer.
Academic Article Tivantinib (ARQ 197) efficacy is independent of MET inhibition in non-small-cell lung cancer cell lines.
Academic Article EPHA2 is a mediator of vemurafenib resistance and a novel therapeutic target in melanoma.
Academic Article Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase.
Academic Article DFG-out mode of inhibition by an irreversible type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors.
Academic Article Protein kinase IKKß-catalyzed phosphorylation of IRF5 at Ser462 induces its dimerization and nuclear translocation in myeloid cells.
Academic Article Identification of novel therapeutic targets in acute leukemias with NRAS mutations using a pharmacologic approach.
Academic Article SnapShot: Kinase Inhibitors II.
Academic Article Systematic analysis of BRAF(V600E) melanomas reveals a role for JNK/c-Jun pathway in adaptive resistance to drug-induced apoptosis.
Academic Article SnapShot: Kinase Inhibitors I.
Academic Article Ligand-associated ERBB2/3 activation confers acquired resistance to FGFR inhibition in FGFR3-dependent cancer cells.
Academic Article A Discovery Strategy for Selective Inhibitors of c-Src in Complex with the Focal Adhesion Kinase SH3/SH2-binding Region.
Academic Article The mitogen-activated protein kinase ERK5 regulates the development and growth of hepatocellular carcinoma.
Academic Article EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors.
Academic Article Development of Selective Covalent Janus Kinase 3 Inhibitors.
Academic Article Extracellular signal-regulated kinase 5 promotes acute cellular and systemic inflammation.
Academic Article Combined EGFR/MEK Inhibition Prevents the Emergence of Resistance in EGFR-Mutant Lung Cancer.
Academic Article YAP Drives Growth by Controlling Transcriptional Pause Release from Dynamic Enhancers.
Academic Article Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells.
Academic Article The ins and outs of selective kinase inhibitor development.
Academic Article Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.
Academic Article Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis.
Academic Article Discovery of a BTK/MNK dual inhibitor for lymphoma and leukemia.
Academic Article EPHA2 Blockade Overcomes Acquired Resistance to EGFR Kinase Inhibitors in Lung Cancer.
Academic Article Inhibition of IKKa by BAY61-3606 Reveals IKKa-Dependent Histone H3 Phosphorylation in Human Cytomegalovirus Infected Cells.
Academic Article NVP-TAE684 reverses multidrug resistance (MDR) in human osteosarcoma by inhibiting P-glycoprotein (PGP1) function.
Academic Article GNF-2 Inhibits Dengue Virus by Targeting Abl Kinases and the Viral E Protein.
Academic Article Discovery of a Highly Selective STK16 Kinase Inhibitor.
Academic Article Pathophysiological significance and therapeutic targeting of germinal center kinase in diffuse large B-cell lymphoma.
Academic Article ALK inhibitor resistance in ALK(F1174L)-driven neuroblastoma is associated with AXL activation and induction of EMT.
Academic Article Salt-Inducible Kinase 2 Couples Ovarian Cancer Cell Metabolism with Survival at the Adipocyte-Rich Metastatic Niche.
Academic Article Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo.
Academic Article Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration.
Academic Article Erk5 Is a Key Regulator of Naive-Primed Transition and Embryonic Stem Cell Identity.
Grant Inhibitors of Kinase Activation
Grant Development and Application of Selective Covalent Cdk7 Inhibitors
Grant Development of covalent PIP4K2 inhibitors for the treatment of p53 deficient lung tumors
Grant Targeting ALK through Degradation and Allosteric Inhibitors
Grant Discovery and optimization of novel mutant-selective allosteric inhibitors of EGFR T790M
Grant Protein Kinase Therapeutic Targets for Non-Small Cell Lung Carcinoma
Grant Developing Selective EphA2 Inhibitors for the treatment of Cancer
Grant Design of inhibitors of drug-resistance protein kinases
Academic Article Covalent Targeting of Fibroblast Growth Factor Receptor Inhibits Metastatic Breast Cancer.
Academic Article Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors.
Academic Article Identification of Existing Drugs That Effectively Target NTRK1 and ROS1 Rearrangements in Lung Cancer.
Academic Article SIKs control osteocyte responses to parathyroid hormone.
Academic Article Inactivation of KLF4 promotes T-cell acute lymphoblastic leukemia and activates the MAP2K7 pathway.
Academic Article Structure-guided development of covalent TAK1 inhibitors.
Academic Article c-Jun N-terminal kinase promotes stem cell phenotype in triple-negative breast cancer through upregulation of Notch1 via activation of c-Jun.
Academic Article Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors.
Academic Article A brain-penetrant RAF dimer antagonist for the noncanonical BRAF oncoprotein of pediatric low-grade astrocytomas.
Academic Article THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors.
Academic Article Leveraging Gas-Phase Fragmentation Pathways for Improved Identification and Selective Detection of Targets Modified by Covalent Probes.
Academic Article 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.
Academic Article Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation.
Academic Article Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model.
Academic Article Small-Molecule Inhibitors of LRRK2.
Academic Article Discovery of a potent dual ALK and EGFR T790M inhibitor.
Academic Article Synergistic interactions with PI3K inhibition that induce apoptosis.
Academic Article A Simple Method to Identify Kinases That Regulate Embryonic Stem Cell Pluripotency by High-throughput Inhibitor Screening.
Academic Article Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.
Academic Article BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment.
Academic Article Vomocytosis of live pathogens from macrophages is regulated by the atypical MAP kinase ERK5.
Academic Article Gemcitabine and Chk1 Inhibitor AZD7762 Synergistically Suppress the Growth of Lkb1-Deficient Lung Adenocarcinoma.
Academic Article Characterization of a highly selective inhibitor of the Aurora kinases.
Academic Article Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells.
Academic Article Dual inhibition of Fes and Flt3 tyrosine kinases potently inhibits Flt3-ITD+ AML cell growth.
Academic Article Progress towards a public chemogenomic set for protein kinases and a call for contributions.
Academic Article Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C.
Grant Targeting the transcriptional and epigenetic landscape in chemo-refractory Small-Cell Lung Cancer
Academic Article Inhibition of USP10 induces degradation of oncogenic FLT3.
Academic Article Enhancer profiling identifies critical cancer genes and characterizes cell identity in adult T-cell leukemia.
Academic Article Activation of the p53 Transcriptional Program Sensitizes Cancer Cells to Cdk7 Inhibitors.
Academic Article CDK4/6 Inhibition Augments Antitumor Immunity by Enhancing T-cell Activation.
Academic Article A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader.
Academic Article Crystal structure of human IRAK1.
Academic Article Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.
Academic Article ER Stress Signaling Promotes the Survival of Cancer "Persister Cells" Tolerant to EGFR Tyrosine Kinase Inhibitors.
Academic Article Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors.
Academic Article BTKCys481Ser drives ibrutinib resistance via ERK1/2 and protects BTKwild-type MYD88-mutated cells by a paracrine mechanism.
Academic Article SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform.
Academic Article ERK5 is activated by oncogenic BRAF and promotes melanoma growth.
Academic Article Kinase inhibitors: the road ahead.
Academic Article Myeloid ERK5 deficiency suppresses tumor growth by blocking protumor macrophage polarization via STAT3 inhibition.
Academic Article Correction: MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells.
Academic Article Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).
Academic Article RAS-MAPK Reactivation Facilitates Acquired Resistance in FGFR1-Amplified Lung Cancer and Underlies a Rationale for Upfront FGFR-MEK Blockade.
Academic Article Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo.
Academic Article Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor.
Academic Article Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors.
Academic Article Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-benzodiazipinones as Inhibitors of Kinases and Bromodomains.
Academic Article First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia.
Academic Article A High-Throughput Immune-Oncology Screen Identifies EGFR Inhibitors as Potent Enhancers of Antigen-Specific Cytotoxic T-lymphocyte Tumor Cell Killing.
Academic Article Targeting the Extracellular Signal-Regulated Kinase 5 Pathway to Suppress Human Chronic Myeloid Leukemia Stem Cells.
Academic Article Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13.
Academic Article A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification.
Academic Article Bruton tyrosine kinase degradation as a therapeutic strategy for cancer.
Academic Article Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML.
Grant Degrading therapeutically important kinases using small molecules
Academic Article Small-molecule targeting of brachyury transcription factor addiction in chordoma.
Academic Article Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor-associated kinase 4 (IRAK4).
Academic Article Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6.
Academic Article Coordinating Tissue Regeneration Through Transforming Growth Factor-ß Activated Kinase 1 Inactivation and Reactivation.
Academic Article A multitargeted probe-based strategy to identify signaling vulnerabilities in cancers.
Academic Article Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome.
Academic Article Cheminformatics Tools for Analyzing and Designing Optimized Small-Molecule Collections and Libraries.
Academic Article Discovery of Covalent CDK14 Inhibitors with Pan-TAIRE Family Specificity.
Academic Article Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype.
Academic Article JNK2 Is Required for the Tumorigenic Properties of Melanoma Cells.
Academic Article What It Takes to Improve a First-Generation Inhibitor to a Second- or Third-Generation Small Molecule.
Academic Article Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor.
Academic Article Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14.
Academic Article Comparison of effects of midostaurin, crenolanib, quizartinib, gilteritinib, sorafenib and BLU-285 on oncogenic mutants of KIT, CBL and FLT3 in haematological malignancies.
Academic Article Pharmacological enhancement of KCC2 gene expression exerts therapeutic effects on human Rett syndrome neurons and Mecp2 mutant mice.
Academic Article BORIS promotes chromatin regulatory interactions in treatment-resistant cancer cells.
Academic Article Synthetic Lethal Interaction of SHOC2 Depletion with MEK Inhibition in RAS-Driven Cancers.
Academic Article Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold.
Academic Article A kinase-independent role for CDK8 in BCR-ABL1+ leukemia.
Academic Article Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation.
Academic Article Salt-inducible kinase inhibition suppresses acute myeloid leukemia progression in vivo.
Academic Article Development and Characterization of a Wee1 Kinase Degrader.
Academic Article Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling.
Academic Article Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells.
Academic Article Exploring Targeted Degradation Strategy for Oncogenic KRASG12C.
Academic Article Treatment-Induced Tumor Dormancy through YAP-Mediated Transcriptional Reprogramming of the Apoptotic Pathway.
Academic Article The combination of FLT3 and SYK kinase inhibitors is toxic to leukaemia cells with CBL mutations.
Academic Article Benzopyrimidodiazepinone inhibitors of TNK2.
Academic Article Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine.
Academic Article Effects of the multi-kinase inhibitor midostaurin in combination with chemotherapy in models of acute myeloid leukaemia.
Academic Article SYK is activated by mutated MYD88 and drives pro-survival signaling in MYD88 driven B-cell lymphomas.
Academic Article Inhibition of the deubiquitinase USP10 induces degradation of SYK.
Academic Article Salt-inducible kinase 1 maintains HDAC7 stability to promote pathologic cardiac remodeling.
Academic Article Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.
Academic Article Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors.
Academic Article Light-induced control of protein destruction by opto-PROTAC.
Academic Article Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors.
Academic Article Discovery of a selective inhibitor of doublecortin like kinase 1.
Academic Article Discovery and Structure-Activity Relationship Study of (Z)-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.
Academic Article Development of CDK2 and CDK5 Dual Degrader TMX-2172.
Academic Article Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13.
Academic Article 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.
Academic Article Structure and Characterization of a Covalent Inhibitor of Src Kinase.
Academic Article Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations.
Academic Article Extracellular-Regulated Protein Kinase 5-Mediated Control of p21 Expression Promotes Macrophage Proliferation Associated with Tumor Growth and Metastasis.
Academic Article Discovery of a series of benzopyrimidodiazepinone TNK2 inhibitors via scaffold morphing.
Academic Article Repurposing of Kinase Inhibitors for Treatment of COVID-19.
Academic Article Catalytic Domain Plasticity of MKK7 Reveals Structural Mechanisms of Allosteric Activation and Diverse Targeting Opportunities.
Academic Article 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".
Academic Article Discovery of Covalent MKK4/7 Dual Inhibitor.
Academic Article Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma.
Academic Article An Embryonic Diapause-like Adaptation with Suppressed Myc Activity Enables Tumor Treatment Persistence.
Academic Article The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification.
Academic Article Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor.
Academic Article Discovery and resistance mechanism of a selective CDK12 degrader.
Academic Article 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.
Academic Article Generation of a chemical genetic model for JAK3.
Academic Article The Cyclin-Dependent Kinase 8 (CDK8) Inhibitor DCA Promotes a Tolerogenic Chemical Immunophenotype in CD4+ T Cells via a Novel CDK8-GATA3-FOXP3 Pathway.
Academic Article INK4 tumor suppressor proteins mediate resistance to CDK4/6 kinase inhibitors.
Academic Article PRM-LIVE with Trapped Ion Mobility Spectrometry and Its Application in Selectivity Profiling of Kinase Inhibitors.
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  • Elongation Factor 2 Kinase
Funded by the NIH National Center for Advancing Translational Sciences through its Clinical and Translational Science Awards Program, grant number UL1TR002541.