Kinase inhibitors: the road ahead

Selectively Targeting the Kinome-Conserved Lysine of PI3Kδ as a General Approach to Covalent Kinase Inhibition

(2018) Samuel E. Dalton et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Achieving neuroprotection with LRRK2 kinase inhibitors in Parkinson disease

(2017) Andrew B. West   EXPERIMENTAL NEUROLOGY

EGFR TKI combination with immunotherapy in non-small cell lung cancer

(2017) Myung-Ju Ahn et al.   Expert Opinion On Drug Safety

Targeting LRRK2 in Parkinson’s disease: an update on recent developments

(2017) Sharon L. Chan et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

3D-e-Chem-VM: Structural Cheminformatics Research Infrastructure in a Freely Available Virtual Machine

(2017) Ross McGuire et al.   Journal of Chemical Information and Modeling

Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design

(2017) Katherine L. Lee et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1

(2017) Andrew P. Crew et al.   JOURNAL OF MEDICINAL CHEMISTRY

Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

(2017) Kwok-Ho Chan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity

(2017) Jack D. Scott et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos

(2017) Mary E. Matyskiela et al.   JOURNAL OF MEDICINAL CHEMISTRY

Protein Degradation via CRL4CRBN Ubiquitin Ligase: Discovery and Structure–Activity Relationships of Novel Glutarimide Analogs That Promote Degradation of Aiolos and/or GSPT1

(2017) Joshua D. Hansen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases

(2017) Philip A. Harris et al.   JOURNAL OF MEDICINAL CHEMISTRY

Kinobead and Single-Shot LC-MS Profiling Identifies Selective PKD Inhibitors

(2017) Martin Golkowski et al.   JOURNAL OF PROTEOME RESEARCH

Predictions of Ligand Selectivity from Absolute Binding Free Energy Calculations

(2017) Matteo Aldeghi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Broad-Spectrum Kinase Profiling in Live Cells with Lysine-Targeted Sulfonyl Fluoride Probes

(2017) Qian Zhao et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

CDK4/6 inhibition triggers anti-tumour immunity

(2017) Shom Goel et al.   NATURE

Global survey of the immunomodulatory potential of common drugs

(2017) Gregory I Vladimer et al.   Nature Chemical Biology

Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells

(2017) Liv Johannessen et al.   Nature Chemical Biology

Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation

(2017) Calla M Olson et al.   Nature Chemical Biology

Structural basis of PROTAC cooperative recognition for selective protein degradation

(2017) Morgan S Gadd et al.   Nature Chemical Biology

Non-kinase targets of protein kinase inhibitors

(2017) Lenka Munoz   NATURE REVIEWS DRUG DISCOVERY

Molecular neurobiology of mTOR

(2017) Katarzyna Switon et al.   NEUROSCIENCE

Redox-based reagents for chemoselective methionine bioconjugation

(2017) Shixian Lin et al.   SCIENCE

The target landscape of clinical kinase drugs

(2017) Susan Klaeger et al.   SCIENCE

Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions

(2017) Tiansheng Wang et al.   ACS Medicinal Chemistry Letters

Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors

(2017) Klemens Hoegenauer et al.   ACS Medicinal Chemistry Letters

Dual leucine zipper kinase-dependent PERK activation contributes to neuronal degeneration following insult

(2017) Martin Larhammar et al.   eLife

Progress towards a public chemogenomic set for protein kinases and a call for contributions

(2017) David H. Drewry et al.   PLoS One

Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model

(2017) Hong Wu et al.   Scientific Reports

Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors

(2016) Susan Klaeger et al.   ACS Chemical Biology

Small-Molecule PROTACS: New Approaches to Protein Degradation

(2016) Momar Toure et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Cancer Immunology and Immunotherapy

(2016) AMMAR SUKARI et al.   ANTICANCER RESEARCH

Computational methods in drug discovery

(2016) Sumudu P Leelananda et al.   Beilstein Journal of Organic Chemistry

Abstract 3025: Discovery of preclinical development candidate inhibitors of the mediator complex-associated kinases CDK8 and CDK19 and evaluation of their therapeutic potential

(2016) Paul Clarke et al.   CANCER RESEARCH

Early Adaptation and Acquired Resistance to CDK4/6 Inhibition in Estrogen Receptor–Positive Breast Cancer

(2016) Maria Teresa Herrera-Abreu et al.   CANCER RESEARCH

Overview of CDK9 as a target in cancer research

(2016) Fatima Morales et al.   CELL CYCLE

EGFR Mutations and ALK Rearrangements Are Associated with Low Response Rates to PD-1 Pathway Blockade in Non-Small Cell Lung Cancer: A Retrospective Analysis

(2016) J. F. Gainor et al.   CLINICAL CANCER RESEARCH

Neuroprotective Mechanisms Mediated by CDK5 Inhibition

(2016) Gohar Mushtaq et al.   CURRENT PHARMACEUTICAL DESIGN

The role of Bruton’s tyrosine kinase in autoimmunity and implications for therapy

(2016) Leslie J. Crofford et al.   Expert Review of Clinical Immunology

MAP Kinase Inhibition Promotes T Cell and Anti-tumor Activity in Combination with PD-L1 Checkpoint Blockade

(2016) Peter J.R. Ebert et al.   IMMUNITY

The Effect of Conformational Flexibility on Binding Free Energy Estimation between Kinases and Their Inhibitors

(2016) Mitsugu Araki et al.   Journal of Chemical Information and Modeling

Selective IRAK4 Inhibition Attenuates Disease in Murine Lupus Models and Demonstrates Steroid Sparing Activity

(2016) Shailesh Dudhgaonkar et al.   JOURNAL OF IMMUNOLOGY

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors

(2016) Philip A. Harris et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy

(2016) Yogesh A. Sonawane et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90–Kinase Interactions

(2016) Meining Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Profiling Prediction of Kinase Inhibitors: Toward the Virtual Assay

(2016) Benjamin Merget et al.   JOURNAL OF MEDICINAL CHEMISTRY

Degradation of Akt using protein-catalyzed capture agents

(2016) Ryan K. Henning et al.   JOURNAL OF PEPTIDE SCIENCE

Metabolically Labile Fumarate Esters Impart Kinetic Selectivity to Irreversible Inhibitors

(2016) Balyn W. Zaro et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Approved and Experimental Small-Molecule Oncology Kinase Inhibitor Drugs: A Mid-2016 Overview

(2016) Peter M. Fischer   MEDICINAL RESEARCH REVIEWS

Proteome-wide covalent ligand discovery in native biological systems

(2016) Keriann M. Backus et al.   NATURE

Overcoming resistance to checkpoint blockade therapy by targeting PI3Kγ in myeloid cells

(2016) Olivier De Henau et al.   NATURE

Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase

(2016) Georg Petzold et al.   NATURE

PI3Kγ is a molecular switch that controls immune suppression

(2016) Megan M. Kaneda et al.   NATURE

Identifying the functional contribution of the defatty-acylase activity of SIRT6

(2016) Xiaoyu Zhang et al.   Nature Chemical Biology

Dynamic undocking and the quasi-bound state as tools for drug discovery

(2016) Sergio Ruiz-Carmona et al.   Nature Chemistry

Targeting focal adhesion kinase renders pancreatic cancers responsive to checkpoint immunotherapy

(2016) Hong Jiang et al.   NATURE MEDICINE

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

Screening out irrelevant cell-based models of disease

(2016) Peter Horvath et al.   NATURE REVIEWS DRUG DISCOVERY

Acquired CDK6 amplification promotes breast cancer resistance to CDK4/6 inhibitors and loss of ER signaling and dependence

(2016) C Yang et al.   ONCOGENE

Activated PI3Kδ syndrome type 2: Two patients, a novel mutation, and review of the literature

(2016) Peter Olbrich et al.   PEDIATRIC ALLERGY AND IMMUNOLOGY

Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds

(2016) Gregory J. Crowther et al.   PLoS One

ERK5 kinase activity is dispensable for cellular immune response and proliferation

(2016) Emme C. K. Lin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The tumor microenvironment underlies acquired resistance to CSF-1R inhibition in gliomas

(2016) D. F. Quail et al.   SCIENCE

Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate

(2016) Catherine A. Evans et al.   ACS Medicinal Chemistry Letters

Discovery of a Series of 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-ones as Selective PI3K-δ/γ Inhibitors

(2016) Fleur M. Ferguson et al.   ACS Medicinal Chemistry Letters

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR

(2016) Timothy P. Heffron et al.   ACS Medicinal Chemistry Letters

Evolution of a New Class of VEGFR-2 Inhibitors from Scaffold Morphing and Redesign

(2016) Nello Mainolfi et al.   ACS Medicinal Chemistry Letters

Selective inhibition of the kinase DYRK1A by targeting its folding process

(2016) Isao Kii et al.   Nature Communications

CDK12 Inhibition Reverses De Novo and Acquired PARP Inhibitor Resistance in BRCA Wild-Type and Mutated Models of Triple-Negative Breast Cancer

(2016) Shawn F. Johnson et al.   Cell Reports

PERK inhibition prevents tau-mediated neurodegeneration in a mouse model of frontotemporal dementia

(2015) Helois Radford et al.   ACTA NEUROPATHOLOGICA

Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL

(2015) Ashton C. Lai et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Could pharmacological curtailment of the RhoA/Rho-kinase pathway reverse the endothelial barrier dysfunction associated with Ebola virus infection?

(2015) Shahram Eisa-Beygi et al.   ANTIVIRAL RESEARCH

Quantifying the Entropy of Binding for Water Molecules in Protein Cavities by Computing Correlations

(2015) David J. Huggins   BIOPHYSICAL JOURNAL

MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells

(2015) L. Beke et al.   BIOSCIENCE REPORTS

Abstract 2698: Combination strategies to target super enhancer transcriptional activity by CDK9 and BRD4 inhibition in acute myeloid leukemia

(2015) Brigham L. Bahr et al.   CANCER RESEARCH

Nuclear FAK Controls Chemokine Transcription, Tregs, and Evasion of Anti-tumor Immunity

(2015) Alan Serrels et al.   CELL

Activity-Based Protein Profiling: Recent Advances in Probe Development and Applications

(2015) Pengyu Yang et al.   CHEMBIOCHEM

Identification and Characterization of an Irreversible Inhibitor of CDK2

(2015) Elizabeth Anscombe et al.   CHEMISTRY & BIOLOGY

Myeloid Cells and Related Chronic Inflammatory Factors as Novel Predictive Markers in Melanoma Treatment with Ipilimumab

(2015) C. Gebhardt et al.   CLINICAL CANCER RESEARCH

The evolution of checkpoint blockade as a cancer therapy: what's here, what's next?

(2015) Daniel Sanghoon Shin et al.   CURRENT OPINION IN IMMUNOLOGY

Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration

(2015) Erik L. Meredith et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials

(2015) Mario Fiore et al.   JOURNAL OF MEDICINAL CHEMISTRY

AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective

(2015) Samuel H. Myers et al.   JOURNAL OF MEDICINAL CHEMISTRY

Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12)

(2015) Snahel Patel et al.   JOURNAL OF MEDICINAL CHEMISTRY

Optimized Chemical Proteomics Assay for Kinase Inhibitor Profiling

(2015) Guillaume Médard et al.   JOURNAL OF PROTEOME RESEARCH

Characterization of Human Cyclin-Dependent Kinase 12 (CDK12) and CDK13 Complexes in C-Terminal Domain Phosphorylation, Gene Transcription, and RNA Processing

(2015) Kaiwei Liang et al.   MOLECULAR AND CELLULAR BIOLOGY

Chromatin-wide Profiling of DYRK1A Reveals a Role as a Gene-Specific RNA Polymerase II CTD Kinase

(2015) Chiara Di Vona et al.   MOLECULAR CELL

Mediator kinase inhibition further activates super-enhancer-associated genes in AML

(2015) Henry E. Pelish et al.   NATURE

Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS

(2015) Jan Krönke et al.   NATURE

A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease

(2015) Trevor Dale et al.   Nature Chemical Biology

Prolonged and tunable residence time using reversible covalent kinase inhibitors

(2015) J Michael Bradshaw et al.   Nature Chemical Biology

The ins and outs of selective kinase inhibitor development

(2015) Susanne Müller et al.   Nature Chemical Biology

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

Translational value of mouse models in oncology drug development

(2015) Stephen E Gould et al.   NATURE MEDICINE

Thermal proteome profiling monitors ligand interactions with cellular membrane proteins

(2015) Friedrich B M Reinhard et al.   NATURE METHODS

Kinase inhibitors and monoclonal antibodies in oncology: clinical implications

(2015) Helen Gharwan et al.   Nature Reviews Clinical Oncology

Tuning kinase inhibitor residence time

(2015) Megan Cully   NATURE REVIEWS DRUG DISCOVERY

Combination cancer immunotherapy and new immunomodulatory targets

(2015) Kathleen M. Mahoney et al.   NATURE REVIEWS DRUG DISCOVERY

Type I/II cytokines, JAKs and new strategies for treating autoimmune diseases

(2015) Daniella M. Schwartz et al.   Nature Reviews Rheumatology

KLIFS: a structural kinase-ligand interaction database

(2015) Albert J. Kooistra et al.   NUCLEIC ACIDS RESEARCH

GPCRdb: an information system for G protein-coupled receptors

(2015) Vignir Isberg et al.   NUCLEIC ACIDS RESEARCH

Immune evasion in cancer: Mechanistic basis and therapeutic strategies

(2015) Dass S. Vinay et al.   SEMINARS IN CANCER BIOLOGY

Sulfonyl fluorides as privileged warheads in chemical biology

(2015) Arjun Narayanan et al.   Chemical Science

Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation

(2015) William T. McElroy et al.   ACS Medicinal Chemistry Letters

Future Therapies of Wet Age-Related Macular Degeneration

(2015) Makoto Ishikawa et al.   Journal of Ophthalmology

Resistance to receptor tyrosine kinase inhibition in cancer: molecular mechanisms and therapeutic strategies

(2015) Peter B. Alexander et al.   Frontiers of Medicine

Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors

(2014) Stuart W. J. Ember et al.   ACS Chemical Biology

Small-Molecule Control of Intracellular Protein Levels through Modulation of the Ubiquitin Proteasome System

(2014) Dennis L. Buckley et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Enzyme Inhibitor Discovery by Activity-Based Protein Profiling

(2014) Micah J. Niphakis et al.   Annual Review of Biochemistry

Targeting Transcriptional Addictions in Small Cell Lung Cancer with a Covalent CDK7 Inhibitor

(2014) Camilla L. Christensen et al.   CANCER CELL

The basal transcription machinery as a target for cancer therapy

(2014) Claudia Villicaña et al.   Cancer Cell International

CDK7 Inhibition Suppresses Super-Enhancer-Linked Oncogenic Transcription in MYCN-Driven Cancer

(2014) Edmond Chipumuro et al.   CELL

Allosteric Inhibition of the IRE1α RNase Preserves Cell Viability and Function during Endoplasmic Reticulum Stress

(2014) Rajarshi Ghosh et al.   CELL

Chemical Interrogation of the Malaria Kinome

(2014) Emily R. Derbyshire et al.   CHEMBIOCHEM

Redox-based probes as tools to monitor oxidized protein tyrosine phosphatases in living cells

(2014) Francisco J. Garcia et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Binding Free-Energy Calculation Is a Powerful Tool for Drug Optimization: Calculation and Measurement of Binding Free Energy for 7-Azaindole Derivatives to Glycogen Synthase Kinase-3β

(2014) Kunihiro Kitamura et al.   Journal of Chemical Information and Modeling

Cutting Edge: RIP1 Kinase Activity Is Dispensable for Normal Development but Is a Key Regulator of Inflammation in SHARPIN-Deficient Mice

(2014) S. B. Berger et al.   JOURNAL OF IMMUNOLOGY

Discovery of Dual Leucine Zipper Kinase (DLK, MAP3K12) Inhibitors with Activity in Neurodegeneration Models

(2014) Snahel Patel et al.   JOURNAL OF MEDICINAL CHEMISTRY

Safety and Efficacy of Tofacitinib, an Oral Janus Kinase Inhibitor, for the Treatment of Rheumatoid Arthritis in Open-label, Longterm Extension Studies

(2014) J. Wollenhaupt et al.   JOURNAL OF RHEUMATOLOGY

Design of Reversible, Cysteine-Targeted Michael Acceptors Guided by Kinetic and Computational Analysis

(2014) Shyam Krishnan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A Novel CDK9 Inhibitor Shows Potent Antitumor Efficacy in Preclinical Hematologic Tumor Models

(2014) T. Yin et al.   MOLECULAR CANCER THERAPEUTICS

Targeting transcription regulation in cancer with a covalent CDK7 inhibitor

(2014) Nicholas Kwiatkowski et al.   NATURE

The E3 ligase Cbl-b and TAM receptors regulate cancer metastasis via natural killer cells

(2014) Magdalena Paolino et al.   NATURE

Inactivation of PI(3)K p110δ breaks regulatory T-cell-mediated immune tolerance to cancer

(2014) Khaled Ali et al.   NATURE

Pharmacological targeting of the pseudokinase Her3

(2014) Ting Xie et al.   Nature Chemical Biology

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

(2014) Pietro Ciceri et al.   Nature Chemical Biology

Covalent docking of large libraries for the discovery of chemical probes

(2014) Nir London et al.   Nature Chemical Biology

A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors

(2014) Bryan R Lanning et al.   Nature Chemical Biology

Idelalisib and Rituximab in Relapsed Chronic Lymphocytic Leukemia

(2014) Richard R. Furman et al.   NEW ENGLAND JOURNAL OF MEDICINE

Crystal structure of EML1 reveals the basis for Hsp90 dependence of oncogenic EML4-ALK by disruption of an atypical  -propeller domain

(2014) M. W. Richards et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Tracking cancer drugs in living cells by thermal profiling of the proteome

(2014) M. M. Savitski et al.   SCIENCE

Myeloid-Derived Suppressor Cells in Cancer: Therapeutic, Predictive, and Prognostic Implications

(2014) C. Marcela Diaz-Montero et al.   SEMINARS IN ONCOLOGY

New Frontiers in Kinases: Special Issue

(2014) Maurizio Botta   ACS Medicinal Chemistry Letters

EML4-ALK Fusions: Propelling Cancer but Creating Exploitable Chaperone Dependence

(2014) P. Workman et al.   Cancer Discovery

Toll-Like Receptor Signaling Pathways

(2014) Takumi Kawasaki et al.   Frontiers in Immunology

Kinase Drug Discovery – What’s Next in the Field?

(2013) Philip Cohen et al.   ACS Chemical Biology

Animal models of CNS disorders

(2013) Paul McGonigle   BIOCHEMICAL PHARMACOLOGY

Targeting IRAK1 as a Therapeutic Approach for Myelodysplastic Syndrome

(2013) Garrett W. Rhyasen et al.   CANCER CELL

Epidermal Growth Factor Receptor-Containing Exosomes Induce Tumor-Specific Regulatory T Cells

(2013) Shao-hong Huang et al.   CANCER INVESTIGATION

Cytotoxic Activity of Tivantinib (ARQ 197) Is Not Due Solely to c-MET Inhibition

(2013) R. Katayama et al.   CANCER RESEARCH

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

Super-Enhancers in the Control of Cell Identity and Disease

(2013) Denes Hnisz et al.   CELL

The CDK-activating kinase Cdk7

(2013) Miriam Merzel Schachter et al.   CELL CYCLE

RNA Polymerase II Transcription Elongation Control

(2013) Jiannan Guo et al.   CHEMICAL REVIEWS

PI3K-δ and PI3K-γ Inhibition by IPI-145 Abrogates Immune Responses and Suppresses Activity in Autoimmune and Inflammatory Disease Models

(2013) David G. Winkler et al.   CHEMISTRY & BIOLOGY

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

Protein kinase inhibitors in the treatment of inflammatory and autoimmune diseases

(2013) H. Patterson et al.   CLINICAL AND EXPERIMENTAL IMMUNOLOGY

Tivantinib (ARQ197) Displays Cytotoxic Activity That Is Independent of Its Ability to Bind MET--Letter

(2013) L. Rimassa et al.   CLINICAL CANCER RESEARCH

Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones

(2013) Xianming Deng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Selective Inhibition of BTK Prevents Murine Lupus and Antibody-Mediated Glomerulonephritis

(2013) A. L. Rankin et al.   JOURNAL OF IMMUNOLOGY

X-ray Crystal Structure of ERK5 (MAPK7) in Complex with a Specific Inhibitor

(2013) Jonathan M. Elkins et al.   JOURNAL OF MEDICINAL CHEMISTRY

Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

(2013) Rand M. Miller et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeting Plasmodium PI(4)K to eliminate malaria

(2013) Case W. McNamara et al.   NATURE

Microenvironmental regulation of tumor progression and metastasis

(2013) Daniela F Quail et al.   NATURE MEDICINE

CSF-1R inhibition alters macrophage polarization and blocks glioma progression

(2013) Stephanie M Pyonteck et al.   NATURE MEDICINE

Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs

(2013) J. Hines et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Explaining why Gleevec is a specific and potent inhibitor of Abl kinase

(2013) Y.-L. Lin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance

(2013) P. A. Schwartz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

(2013) D. M. Molina et al.   SCIENCE

Death of a Titan

(2013) M. Sudol et al.   Science Signaling

Oral Treatment Targeting the Unfolded Protein Response Prevents Neurodegeneration and Clinical Disease in Prion-Infected Mice

(2013) J. A. Moreno et al.   Science Translational Medicine

Targeted Inhibition of the Molecular Chaperone Hsp90 Overcomes ALK Inhibitor Resistance in Non–Small Cell Lung Cancer

(2013) Jim Sang et al.   Cancer Discovery

Activation of the PD-1 Pathway Contributes to Immune Escape in EGFR-Driven Lung Tumors

(2013) E. A. Akbay et al.   Cancer Discovery

CDK8-Mediated STAT1-S727 Phosphorylation Restrains NK Cell Cytotoxicity and Tumor Surveillance

(2013) Eva Maria Putz et al.   Cell Reports

Bruton’s Tyrosine Kinase (BTK) Inhibitors in Clinical Trials

(2013) Jan A. Burger   Current Hematologic Malignancy Reports

c-Myc Is a Universal Amplifier of Expressed Genes in Lymphocytes and Embryonic Stem Cells

(2012) Zuqin Nie et al.   CELL

Chemistry-based functional proteomics for drug target deconvolution

(2012) Kui Wang et al.   Expert Review of Proteomics

Plasmodiumkinases as targets for new-generation antimalarials

(2012) Isabelle S Lucet et al.   Future Medicinal Chemistry

Life Beyond Kinases: Structure-Based Discovery of Sorafenib as Nanomolar Antagonist of 5-HT Receptors

(2012) Xingyu Lin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK)

(2012) Jeffrey M. Axten et al.   JOURNAL OF MEDICINAL CHEMISTRY

Ranibizumab Combined With Low-Dose Sorafenib for Exudative Age-Related Macular Degeneration

(2012) Teresa Diago et al.   MAYO CLINIC PROCEEDINGS

Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles

(2012) Iana M Serafimova et al.   Nature Chemical Biology

Mutations in UVSSA cause UV-sensitive syndrome and destabilize ERCC6 in transcription-coupled DNA repair

(2012) Xue Zhang et al.   NATURE GENETICS

AXL and acquired resistance to EGFR inhibitors

(2012) Sophie Postel-Vinay et al.   NATURE GENETICS

Drug repositioning for Alzheimer's disease

(2012) Anne Corbett et al.   NATURE REVIEWS DRUG DISCOVERY

Mechanisms of Age-Related Macular Degeneration

(2012) Jayakrishna Ambati et al.   NEURON

Placebo-Controlled Trial of Tofacitinib Monotherapy in Rheumatoid Arthritis

(2012) Roy Fleischmann et al.   NEW ENGLAND JOURNAL OF MEDICINE

Safety and Activity of Anti–PD-L1 Antibody in Patients with Advanced Cancer

(2012) Julie R. Brahmer et al.   NEW ENGLAND JOURNAL OF MEDICINE

Sphingosine kinase 1 in viral infections

(2012) Jillian M. Carr et al.   REVIEWS IN MEDICAL VIROLOGY

Redox-Based Probes for Protein Tyrosine Phosphatases

(2011) Stephen E. Leonard et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Receptor Tyrosine Kinases and Targeted Cancer Therapeutics

(2011) Kenji Takeuchi et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Receptor Tyrosine Kinases and TLR/IL1Rs Unexpectedly Activate Myeloid Cell PI3Kγ, A Single Convergent Point Promoting Tumor Inflammation and Progression

(2011) Michael C. Schmid et al.   CANCER CELL

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

In Situ Kinase Profiling Reveals Functionally Relevant Properties of Native Kinases

(2011) Matthew P. Patricelli et al.   CHEMISTRY & BIOLOGY

High-Throughput Kinase Profiling: A More Efficient Approach toward the Discovery of New Kinase Inhibitors

(2011) Chandrasekhar V. Miduturu et al.   CHEMISTRY & BIOLOGY

New Frontiers in Chemical Biology: Enabling Drug Discovery. Edited by Mark E. Bunnage.

(2011) Joshua Kritzer   ChemMedChem

Mechanisms of drug resistance in kinases

(2011) Rina Barouch-Bentov et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Role of LRRK2 kinase dysfunction in Parkinson disease

(2011) Azad Kumar et al.   EXPERT REVIEWS IN MOLECULAR MEDICINE

Inhibition of Focal Adhesion Kinase by PF-562,271 Inhibits the Growth and Metastasis of Pancreatic Cancer Concomitant with Altering the Tumor Microenvironment

(2011) J. B. Stokes et al.   MOLECULAR CANCER THERAPEUTICS

IC261 induces cell cycle arrest and apoptosis of human cancer cells via CK1δ/ɛ and Wnt/β-catenin independent inhibition of mitotic spindle formation

(2011) J K Cheong et al.   ONCOGENE

Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK

(2011) R. Katayama et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Isoform-specific regulation of Akt by PDGF-induced reactive oxygen species

(2011) R. Wani et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1

(2011) Xianming Deng et al.   ACS Medicinal Chemistry Letters

Inhibition of ALK, PI3K/MEK, and HSP90 in Murine Lung Adenocarcinoma Induced by EML4-ALK Fusion Oncogene

(2010) Z. Chen et al.   CANCER RESEARCH

Understanding Kinase Selectivity Through Energetic Analysis of Binding Site Waters

(2010) Daniel D. Robinson et al.   ChemMedChem

Signaling cell death from the endoplasmic reticulum stress response

(2010) Gordon C Shore et al.   CURRENT OPINION IN CELL BIOLOGY

The (un)targeted cancer kinome

(2010) Oleg Fedorov et al.   Nature Chemical Biology

An Oral Spleen Tyrosine Kinase (Syk) Inhibitor for Rheumatoid Arthritis

(2010) Michael E. Weinblatt et al.   NEW ENGLAND JOURNAL OF MEDICINE

Leucine-Rich Repeat Kinase 2 Mutations and Parkinson's Disease: Three Questions

(2009) Elisa Greggio et al.   ASN Neuro

Neutralization of Vascular Endothelial Growth Factor Antiangiogenic Isoforms Is More Effective Than Treatment with Proangiogenic Isoforms in Stimulating Vascular Development and Follicle Progression in the Perinatal Rat Ovary1

(2009) Robin A. Artac et al.   BIOLOGY OF REPRODUCTION

IRE1α Kinase Activation Modes Control Alternate Endoribonuclease Outputs to Determine Divergent Cell Fates

(2009) Dan Han et al.   CELL

Targeting protein kinases for the development of anti-inflammatory drugs

(2009) Philip Cohen   CURRENT OPINION IN CELL BIOLOGY

Protein kinases as antibacterial targets

(2009) Mark Schreiber et al.   CURRENT OPINION IN CELL BIOLOGY

Vinyl sulfone: a versatile function for simple bioconjugation and immobilization

(2009) Julia Morales-Sanfrutos et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

An orally bioavailable spleen tyrosine kinase inhibitor delays disease progression and prolongs survival in murine lupus

(2008) Frances Rena Bahjat et al.   ARTHRITIS AND RHEUMATISM

Imatinib resistance in CML

(2008) Gisella Volpe et al.   CANCER LETTERS

Role of the Active-Site Solvent in the Thermodynamics of Factor Xa Ligand Binding

(2008) Robert Abel et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Phenotype, genotype, and worldwide genetic penetrance of LRRK2-associated Parkinson's disease: a case-control study

(2008) Daniel G Healy et al.   LANCET NEUROLOGY

High-throughput kinase profiling as a platform for drug discovery

(2008) David M. Goldstein et al.   NATURE REVIEWS DRUG DISCOVERY