相关参考文献
注意:仅列出部分参考文献,下载原文获取全部文献信息。Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1
Andrew P. Crew et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
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
Kwok-Ho Chan et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos
Mary E. Matyskiela et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Protein Degradation via CRL4CRBN Ubiquitin Ligase: Discovery and Structure-Activity Relationships of Novel Glutarimide Analogs That Promote Degradation of Aiolos and/or GSPT1
Joshua D. Hansen et al.
JOURNAL OF MEDICINAL CHEMISTRY (2018)
Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation
Calla M. Olson et al.
NATURE CHEMICAL BIOLOGY (2018)
Selectively Targeting the Kinome-Conserved Lysine of PI3Kδ as a General Approach to Covalent Kinase Inhibition
Samuel E. Dalton et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2018)
A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader
Hai-Tsang Huang et al.
CELL CHEMICAL BIOLOGY (2018)
Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead
Daniel P. Bondeson et al.
CELL CHEMICAL BIOLOGY (2018)
Selective IRAK4 Inhibition Attenuates Disease in Murine Lupus Models and Demonstrates Steroid Sparing Activity
Shailesh Dudhgaonkar et al.
JOURNAL OF IMMUNOLOGY (2017)
Profiling Prediction of Kinase Inhibitors: Toward the Virtual Assay
Benjamin Merget et al.
JOURNAL OF MEDICINAL CHEMISTRY (2017)
Approved and Experimental Small-Molecule Oncology Kinase Inhibitor Drugs: A Mid-2016 Overview
Peter M. Fischer
MEDICINAL RESEARCH REVIEWS (2017)
Dynamic undocking and the quasi-bound state as tools for drug discovery
Sergio Ruiz-Carmona et al.
NATURE CHEMISTRY (2017)
Induced protein degradation: an emerging drug discovery paradigm
Ashton C. Lai et al.
NATURE REVIEWS DRUG DISCOVERY (2017)
Acquired CDK6 amplification promotes breast cancer resistance to CDK4/6 inhibitors and loss of ER signaling and dependence
C. Yang et al.
ONCOGENE (2017)
Achieving neuroprotection with LRRK2 kinase inhibitors in Parkinson disease
Andrew B. West
EXPERIMENTAL NEUROLOGY (2017)
EGFR TKI combination with immunotherapy in non-small cell lung cancer
Myung-Ju Ahn et al.
EXPERT OPINION ON DRUG SAFETY (2017)
Targeting LRRK2 in Parkinson's disease: an update on recent developments
Sharon L. Chan et al.
EXPERT OPINION ON THERAPEUTIC TARGETS (2017)
3D-e-Chem-VM: Structural Cheminformatics Research Infrastructure in a Freely Available Virtual Machine
Ross McGuire et al.
JOURNAL OF CHEMICAL INFORMATION AND MODELING (2017)
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
Katherine L. Lee et al.
JOURNAL OF MEDICINAL CHEMISTRY (2017)
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
Jack D. Scott et al.
JOURNAL OF MEDICINAL CHEMISTRY (2017)
Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases
Philip A. Harris et al.
JOURNAL OF MEDICINAL CHEMISTRY (2017)
Kinobead and Single-Shot LC-MS Profiling Identifies Selective PKD Inhibitors
Martin Golkowski et al.
JOURNAL OF PROTEOME RESEARCH (2017)
Predictions of Ligand Selectivity from Absolute Binding Free Energy Calculations
Matteo Aldeghi et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2017)
Broad-Spectrum Kinase Profiling in Live Cells with Lysine-Targeted Sulfonyl Fluoride Probes
Qian Zhao et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2017)
CDK4/6 inhibition triggers anti-tumour immunity
Shom Goel et al.
NATURE (2017)
Global survey of the immunomodulatory potential of common drugs
Gregory I. Vladimer et al.
NATURE CHEMICAL BIOLOGY (2017)
Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells
Liv Johannessen et al.
NATURE CHEMICAL BIOLOGY (2017)
Structural basis of PROTAC cooperative recognition for selective protein degradation
Morgan S. Gadd et al.
NATURE CHEMICAL BIOLOGY (2017)
Non-kinase targets of protein kinase inhibitors
Lenka Munoz
NATURE REVIEWS DRUG DISCOVERY (2017)
Redox-based reagents for chemoselective methionine bioconjugation
Shixian Lin et al.
SCIENCE (2017)
The target landscape of clinical kinase drugs
Susan Klaeger et al.
SCIENCE (2017)
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions
Tiansheng Wang et al.
ACS MEDICINAL CHEMISTRY LETTERS (2017)
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors
Klemens Hoegenauer et al.
ACS MEDICINAL CHEMISTRY LETTERS (2017)
Dual leucine zipper kinase-dependent PERK activation contributes to neuronal degeneration following insult
Martin Larhammar et al.
ELIFE (2017)
Progress towards a public chemogenomic set for protein kinases and a call for contributions
David H. Drewry et al.
PLOS ONE (2017)
Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model
Hong Wu et al.
SCIENTIFIC REPORTS (2017)
Effective activated PI3Kδ syndrome-targeted therapy with the PI3Kd inhibitor leniolisib
V. Koneti Rao et al.
BLOOD (2017)
Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC)
Caroline M. Robb et al.
CHEMICAL COMMUNICATIONS (2017)
Proteasome Activation by Small Molecules
Yves Leestemaker et al.
CELL CHEMICAL BIOLOGY (2017)
Mechanisms and consequences of Jak-STAT signaling in the immune system
Alejandro V. Villarino et al.
NATURE IMMUNOLOGY (2017)
Development of Potent, Selective SRPK1 Inhibitors as Potential Topical Therapeutics for Neovascular Eye Disease
Jennifer Batson et al.
ACS CHEMICAL BIOLOGY (2017)
Transcriptional Addiction in Cancer
James E. Bradner et al.
CELL (2017)
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL
Ashton C. Lai et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2016)
Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials
Mario Fiore et al.
JOURNAL OF MEDICINAL CHEMISTRY (2016)
AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective
Samuel H. Myers et al.
JOURNAL OF MEDICINAL CHEMISTRY (2016)
Kinase inhibitors and monoclonal antibodies in oncology: clinical implications
Helen Gharwan et al.
NATURE REVIEWS CLINICAL ONCOLOGY (2016)
Type I/II cytokines, JAKs, and new strategies for treating autoimmune diseases
Daniella M. Schwartz et al.
NATURE REVIEWS RHEUMATOLOGY (2016)
KLIFS: a structural kinase-ligand interaction database
Albert J. Kooistra et al.
NUCLEIC ACIDS RESEARCH (2016)
GPCRdb: an information system for G protein-coupled receptors
Vignir Isberg et al.
NUCLEIC ACIDS RESEARCH (2016)
Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors
Susan Klaeger et al.
ACS CHEMICAL BIOLOGY (2016)
Small-Molecule PROTACS: New Approaches to Protein Degradation
Momar Toure et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2016)
Computational methods in drug discovery
Sumudu P. Leelananda et al.
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY (2016)
Discovery of preclinical development candidate inhibitors of the mediator complex-associated kinases CDK8 and CDK19 and evaluation of their therapeutic potential
Paul Clarke et al.
CANCER RESEARCH (2016)
Early Adaptation and Acquired Resistance to CDK4/6 Inhibition in Estrogen Receptor-Positive Breast Cancer
Maria Teresa Herrera-Abreu et al.
CANCER RESEARCH (2016)
Overview of CDK9 as a target in cancer research
Fatima Morales et al.
CELL CYCLE (2016)
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
Justin F. Gainor et al.
CLINICAL CANCER RESEARCH (2016)
Neuroprotective Mechanisms Mediated by CDK5 Inhibition
Gohar Mushtaq et al.
CURRENT PHARMACEUTICAL DESIGN (2016)
The role of Bruton's tyrosine kinase in autoimmunity and implications for therapy
Leslie J. Crofford et al.
EXPERT REVIEW OF CLINICAL IMMUNOLOGY (2016)
MAP Kinase Inhibition Promotes T Cell and Anti-tumor Activity in Combination with PD-L1 Checkpoint Blockade
Peter J. R. Ebert et al.
IMMUNITY (2016)
The Effect of Conformational Flexibility on Binding Free Energy Estimation between Kinases and Their Inhibitors
Mitsugu Araki et al.
JOURNAL OF CHEMICAL INFORMATION AND MODELING (2016)
DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors
Philip A. Harris et al.
JOURNAL OF MEDICINAL CHEMISTRY (2016)
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy
Yogesh A. Sonawane et al.
JOURNAL OF MEDICINAL CHEMISTRY (2016)
Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions
Meining Wang et al.
JOURNAL OF MEDICINAL CHEMISTRY (2016)
Degradation of Akt using protein-catalyzed capture agents
Ryan K. Henning et al.
JOURNAL OF PEPTIDE SCIENCE (2016)
Metabolically Labile Fumarate Esters Impart Kinetic Selectivity to Irreversible Inhibitors
Balyn W. Zaro et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2016)
Proteome-wide covalent ligand discovery in native biological systems
Keriann M. Backus et al.
NATURE (2016)
Overcoming resistance to checkpoint blockade therapy by targeting PI3Kγ in myeloid cells
Olivier De Henau et al.
NATURE (2016)
Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase
Georg Petzold et al.
NATURE (2016)
PI3Kγ is a molecular switch that controls immune suppression
Megan M. Kaneda et al.
NATURE (2016)
Identifying the functional contribution of the defatty-acylase activity of SIRT6
Xiaoyu Zhang et al.
Nature Chemical Biology (2016)
Targeting focal adhesion kinase renders pancreatic cancers responsive to checkpoint immunotherapy
Hong Jiang et al.
NATURE MEDICINE (2016)
Screening out irrelevant cell-based models of disease
Peter Horvath et al.
NATURE REVIEWS DRUG DISCOVERY (2016)
Activated PI3Kδ syndrome type 2: Two patients, a novel mutation, and review of the literature
Peter Olbrich et al.
PEDIATRIC ALLERGY AND IMMUNOLOGY (2016)
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds
Gregory J. Crowther et al.
PLOS ONE (2016)
ERK5 kinase activity is dispensable for cellular immune response and proliferation
Emme C. K. Lin et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2016)
The tumor microenvironment underlies acquired resistance to CSF-1R inhibition in gliomas
Daniela F. Quail et al.
SCIENCE (2016)
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate
Catherine A. Evans et al.
ACS MEDICINAL CHEMISTRY LETTERS (2016)
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
Fleur M. Ferguson et al.
ACS MEDICINAL CHEMISTRY LETTERS (2016)
Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR
Timothy P. Heffron et al.
ACS MEDICINAL CHEMISTRY LETTERS (2016)
Evolution of a New Class of VEGFR-2 Inhibitors from Scaffold Morphing and Redesign
Nello Mainolfi et al.
ACS MEDICINAL CHEMISTRY LETTERS (2016)
Selective inhibition of the kinase DYRK1A by targeting its folding process
Isao Kii et al.
NATURE COMMUNICATIONS (2016)
CDK12 Inhibition Reverses De Novo and Acquired PARP Inhibitor Resistance in BRCA Wild-Type and Mutated Models of Triple-Negative Breast Cancer
Shawn F. Johnson et al.
CELL REPORTS (2016)
ERK5 and Cell Proliferation: Nuclear Localization Is What Matters
Nestor Gomez et al.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY (2016)
GNF-2 Inhibits Dengue Virus by Targeting Abl Kinases and the Viral E Protein
Margaret J. Clark et al.
CELL CHEMICAL BIOLOGY (2016)
Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket
Michael Forster et al.
CELL CHEMICAL BIOLOGY (2016)
PERK inhibition prevents tau-mediated neurodegeneration in a mouse model of frontotemporal dementia
Helois Radford et al.
ACTA NEUROPATHOLOGICA (2015)
Could pharmacological curtailment of the RhoA/Rho-kinase pathway reverse the endothelial barrier dysfunction associated with Ebola virus infection?
Shahram Eisa-Beygi et al.
ANTIVIRAL RESEARCH (2015)
Quantifying the Entropy of Binding for Water Molecules in Protein Cavities by Computing Correlations
David J. Huggins
BIOPHYSICAL JOURNAL (2015)
MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells
Lijs Beke et al.
BIOSCIENCE REPORTS (2015)
Combination strategies to target super enhancer transcriptional activity by CDK9 and BRD4 inhibition in acute myeloid leukemia
Brigham L. Bahr et al.
CANCER RESEARCH (2015)
Nuclear FAK Controls Chemokine Transcription, Tregs, and Evasion of Anti-tumor Immunity
Alan Serrels et al.
CELL (2015)
Activity-Based Protein Profiling: Recent Advances in Probe Development and Applications
Pengyu Yang et al.
CHEMBIOCHEM (2015)
Identification and Characterization of an Irreversible Inhibitor of CDK2
Elizabeth Anscombe et al.
CHEMISTRY & BIOLOGY (2015)
Myeloid Cells and Related Chronic Inflammatory Factors as Novel Predictive Markers in Melanoma Treatment with Ipilimumab
Christoffer Gebhardt et al.
CLINICAL CANCER RESEARCH (2015)
The evolution of checkpoint blockade as a cancer therapy: what's here, what's next?
Daniel Sanghoon Shin et al.
CURRENT OPINION IN IMMUNOLOGY (2015)
Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration
Erik L. Meredith et al.
JOURNAL OF MEDICINAL CHEMISTRY (2015)
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)
Snahel Patel et al.
JOURNAL OF MEDICINAL CHEMISTRY (2015)
Optimized Chemical Proteomics Assay for Kinase Inhibitor Profiling
Guillaume Medard et al.
JOURNAL OF PROTEOME RESEARCH (2015)
Characterization of Human Cyclin-Dependent Kinase 12 (CDK12) and CDK13 Complexes in C-Terminal Domain Phosphorylation, Gene Transcription, and RNA Processing
Kaiwei Liang et al.
MOLECULAR AND CELLULAR BIOLOGY (2015)
Chromatin-wide Profiling of DYRK1A Reveals a Role as a Gene-Specific RNA Polymerase II CTD Kinase
Chiara Di Vona et al.
MOLECULAR CELL (2015)
Mediator kinase inhibition further activates super-enhancer-associated genes in AML
Henry E. Pelish et al.
NATURE (2015)
Lenalidomide induces ubiquitination and degradation of CK1a in del(5q) MDS
Jan Kroenke et al.
NATURE (2015)
A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease
Trevor Dale et al.
NATURE CHEMICAL BIOLOGY (2015)
Prolonged and tunable residence time using reversible covalent kinase inhibitors
J. Michael Bradshaw et al.
NATURE CHEMICAL BIOLOGY (2015)
The ins and outs of selective kinase inhibitor development
Susanne Mueller et al.
NATURE CHEMICAL BIOLOGY (2015)
Catalytic in vivo protein knockdown by small-molecule PROTACs
Daniel P. Bondeson et al.
NATURE CHEMICAL BIOLOGY (2015)
Translational value of mouse models in oncology drug development
Stephen E. Gould et al.
NATURE MEDICINE (2015)
Thermal proteome profiling monitors ligand interactions with cellular membrane proteins
Friedrich B. M. Reinhard et al.
NATURE METHODS (2015)
Tuning kinase inhibitor residence time
Megan Cully
NATURE REVIEWS DRUG DISCOVERY (2015)
Combination cancer immunotherapy and new immunomodulatory targets
Kathleen M. Mahoney et al.
NATURE REVIEWS DRUG DISCOVERY (2015)
Immune evasion in cancer: Mechanistic basis and therapeutic strategies
Dass S. Vinay et al.
SEMINARS IN CANCER BIOLOGY (2015)
Sulfonyl fluorides as privileged warheads in chemical biology
Arjun Narayanan et al.
CHEMICAL SCIENCE (2015)
Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation
William T. McElroy et al.
ACS MEDICINAL CHEMISTRY LETTERS (2015)
Future Therapies of Wet Age-Related Macular Degeneration
Makoto Ishikawa et al.
JOURNAL OF OPHTHALMOLOGY (2015)
Resistance to receptor tyrosine kinase inhibition in cancer: molecular mechanisms and therapeutic strategies
Peter B. Alexander et al.
FRONTIERS OF MEDICINE (2015)
Discovery of Dual Leucine Zipper Kinase (DLK, MAP3K12) Inhibitors with Activity in Neurodegeneration Models
Snahel Patel et al.
JOURNAL OF MEDICINAL CHEMISTRY (2015)
Directly targeting transcriptional dysregulation in cancer
Thomas J. Gonda et al.
NATURE REVIEWS CANCER (2015)
Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors
Stuart W. J. Ember et al.
ACS CHEMICAL BIOLOGY (2014)
Small-Molecule Control of Intracellular Protein Levels through Modulation of the Ubiquitin Proteasome System
Dennis L. Buckley et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2014)
Enzyme Inhibitor Discovery by Activity-Based Protein Profiling
Micah J. Niphakis et al.
ANNUAL REVIEW OF BIOCHEMISTRY, VOL 83 (2014)
Animal models of CNS disorders
Paul McGonigle
BIOCHEMICAL PHARMACOLOGY (2014)
Targeting Transcriptional Addictions in Small Cell Lung Cancer with a Covalent CDK7 Inhibitor
Camilla L. Christensen et al.
CANCER CELL (2014)
The basal transcription machinery as a target for cancer therapy
Claudia Villicana et al.
CANCER CELL INTERNATIONAL (2014)
CDK7 Inhibition Suppresses Super-Enhancer-Linked Oncogenic Transcription in MYCN-Driven Cancer
Edmond Chipumuro et al.
CELL (2014)
Allosteric Inhibition of the IRE1α RNase Preserves Cell Viability and Function during Endoplasmic Reticulum Stress
Rajarshi Ghosh et al.
CELL (2014)
Chemical Interrogation of the Malaria Kinome
Emily R. Derbyshire et al.
CHEMBIOCHEM (2014)
Protein kinase inhibitors in the treatment of inflammatory and autoimmune diseases
H. Patterson et al.
CLINICAL AND EXPERIMENTAL IMMUNOLOGY (2014)
Redox-based probes as tools to monitor oxidized protein tyrosine phosphatases in living cells
Francisco J. Garcia et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2014)
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
Kunihiro Kitamura et al.
JOURNAL OF CHEMICAL INFORMATION AND MODELING (2014)
Cutting Edge: RIP1 Kinase Activity Is Dispensable for Normal Development but Is a Key Regulator of Inflammation in SHARPIN-Deficient Mice
Scott B. Berger et al.
JOURNAL OF IMMUNOLOGY (2014)
Safety and Efficacy of Tofacitinib, an Oral Janus Kinase Inhibitor, for the Treatment of Rheumatoid Arthritis in Open-label, Longterm Extension Studies
Juergen Wollenhaupt et al.
JOURNAL OF RHEUMATOLOGY (2014)
Design of Reversible, Cysteine-Targeted Michael Acceptors Guided by Kinetic and Computational Analysis
Shyam Krishnan et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2014)
A Novel CDK9 Inhibitor Shows Potent Antitumor Efficacy in Preclinical Hematologic Tumor Models
Tinggui Yin et al.
MOLECULAR CANCER THERAPEUTICS (2014)
Targeting transcription regulation in cancer with a covalent CDK7 inhibitor
Nicholas Kwiatkowski et al.
NATURE (2014)
The E3 ligase Cbl-b and TAM receptors regulate cancer metastasis via natural killer cells
Magdalena Paolino et al.
NATURE (2014)
Inactivation of PI(3)K p110δ breaks regulatory T-cell-mediated immune tolerance to cancer
Khaled Ali et al.
NATURE (2014)
Pharmacological targeting of the pseudokinase Her3
Ting Xie et al.
NATURE CHEMICAL BIOLOGY (2014)
Dual kinase-bromodomain inhibitors for rationally designed polypharmacology
Pietro Ciceri et al.
NATURE CHEMICAL BIOLOGY (2014)
Covalent docking of large libraries for the discovery of chemical probes
Nir London et al.
NATURE CHEMICAL BIOLOGY (2014)
A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors
Bryan R. Lannine et al.
NATURE CHEMICAL BIOLOGY (2014)
Idelalisib and Rituximab in Relapsed Chronic Lymphocytic Leukemia
Richard R. Furman et al.
NEW ENGLAND JOURNAL OF MEDICINE (2014)
Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance
Phillip A. Schwartz et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2014)
Crystal structure of EML1 reveals the basis for Hsp90 dependence of oncogenic EML4-ALK by disruption of an atypical β-propeller domain
Mark W. Richards et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2014)
Tracking cancer drugs in living cells by thermal profiling of the proteome
Mikhail M. Savitski et al.
SCIENCE (2014)
Myeloid-Derived Suppressor Cells in Cancer: Therapeutic, Predictive, and Prognostic Implications
C. Marcelo Diaz-Montero et al.
SEMINARS IN ONCOLOGY (2014)
New Frontiers in Kinases: Special Issue
Maurizio Botta
ACS MEDICINAL CHEMISTRY LETTERS (2014)
EML4-ALK Fusions: Propelling Cancer but Creating Exploitable Chaperone Dependence
Paul Workman et al.
CANCER DISCOVERY (2014)
Bruton's Tyrosine Kinase (BTK) Inhibitors in Clinical Trials
Jan A. Burger
CURRENT HEMATOLOGIC MALIGNANCY REPORTS (2014)
Toll-like receptor signaling pathways
Takumi Kawasaki et al.
FRONTIERS IN IMMUNOLOGY (2014)
Novel Phosphoinositide 3-Kinase δ,γ Inhibitor: Potent Anti-Inflammatory Effects and Joint Protection in Models of Rheumatoid Arthritis
David L. Boyle et al.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2014)
Kinase Drug Discovery - What's Next in the Field?
Philip Cohen et al.
ACS CHEMICAL BIOLOGY (2013)
Targeting IRAK1 as a Therapeutic Approach for Myelodysplastic Syndrome
Garrett W. Rhyasen et al.
CANCER CELL (2013)
Epidermal Growth Factor Receptor-Containing Exosomes Induce Tumor-Specific Regulatory T Cells
Shao-hong Huang et al.
CANCER INVESTIGATION (2013)
Cytotoxic Activity of Tivantinib (ARQ 197) Is Not Due Solely to c-MET Inhibition
Ryohei Katayama et al.
CANCER RESEARCH (2013)
Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers
Jakob Loven et al.
CELL (2013)
Super-Enhancers in the Control of Cell Identity and Disease
Denes Hnisz et al.
CELL (2013)
The CDK-activating kinase Cdk7 Taking yes for an answer
Miriam Merzel Schachter et al.
CELL CYCLE (2013)
RNA Polymerase II Transcription Elongation Control
Jiannan Guo et al.
CHEMICAL REVIEWS (2013)
PI3K-δ and PI3K-γ Inhibition by IPI-145 Abrogates Immune Responses and Suppresses Activity in Autoimmune and Inflammatory Disease Models
David G. Winkler et al.
CHEMISTRY & BIOLOGY (2013)
Developing Irreversible Inhibitors of the Protein Kinase Cysteinome
Qingsong Liu et al.
CHEMISTRY & BIOLOGY (2013)
Tivantinib (ARQ197) Displays Cytotoxic Activity That Is Independent of Its Ability to Bind MET-Letter
Lorenza Rimassa et al.
CLINICAL CANCER RESEARCH (2013)
Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones
Xianming Deng et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2013)
Selective Inhibition of BTK Prevents Murine Lupus and Antibody-Mediated Glomerulonephritis
Andrew L. Rankin et al.
JOURNAL OF IMMUNOLOGY (2013)
X-ray Crystal Structure of ERK5 (MAPK7) in Complex with a Specific Inhibitor
Jonathan M. Elkins et al.
JOURNAL OF MEDICINAL CHEMISTRY (2013)
Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors
Rand M. Miller et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2013)
Targeting Plasmodium PI(4)K to eliminate malaria
Case W. McNamara et al.
NATURE (2013)
Microenvironmental regulation of tumor progression and metastasis
Daniela F. Quail et al.
NATURE MEDICINE (2013)
CSF-1R inhibition alters macrophage polarization and blocks glioma progression
Stephanie M. Pyonteck et al.
NATURE MEDICINE (2013)
Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs
John Hines et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2013)
Explaining why Gleevec is a specific and potent inhibitor of Abl kinase
Yen-Lin Lin et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2013)
Sphingosine kinase 1 in viral infections
Jillian M. Carr et al.
REVIEWS IN MEDICAL VIROLOGY (2013)
Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay
Daniel Martinez Molina et al.
SCIENCE (2013)
Death of a Titan
Marius Sudol et al.
SCIENCE SIGNALING (2013)
Oral Treatment Targeting the Unfolded Protein Response Prevents Neurodegeneration and Clinical Disease in Prion-Infected Mice
Julie A. Moreno et al.
SCIENCE TRANSLATIONAL MEDICINE (2013)
Targeted Inhibition of the Molecular Chaperone Hsp90 Overcomes ALK Inhibitor Resistance in Non-Small Cell Lung Cancer
Jim Sang et al.
CANCER DISCOVERY (2013)
Activation of the PD-1 Pathway Contributes to Immune Escape in EGFR-Driven Lung Tumors
Esra A. Akbay et al.
CANCER DISCOVERY (2013)
CDK8-Mediated STAT1-S727 Phosphorylation Restrains NK Cell Cytotoxicity and Tumor Surveillance
Eva Maria Putz et al.
CELL REPORTS (2013)
Inhibition of Btk with CC-292 Provides Early Pharmacodynamic Assessment of Activity in Mice and Humans
Erica K. Evans et al.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2013)
Lectin Microarray Profiling and Relative Quantification of Glycome Associated With Proteins of Neonatal wt and rd1 Mice Retinae
Satpal Ahuja
INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE (2013)
Dysregulation of the basal RNA polymerase transcription apparatus in cancer
Megan J. Bywater et al.
NATURE REVIEWS CANCER (2013)
c-Myc Is a Universal Amplifier of Expressed Genes in Lymphocytes and Embryonic Stem Cells
Zuqin Nie et al.
CELL (2012)
Chemistry-based functional proteomics for drug target deconvolution
Kui Wang et al.
EXPERT REVIEW OF PROTEOMICS (2012)
Plasmodium kinases as targets for new-generation antimalarials
Isabelle S. Lucet et al.
FUTURE MEDICINAL CHEMISTRY (2012)
Life Beyond Kinases: Structure-Based Discovery of Sorafenib as Nanomolar Antagonist of 5-HT Receptors
Xingyu Lin et al.
JOURNAL OF MEDICINAL CHEMISTRY (2012)
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)
Jeffrey M. Axten et al.
JOURNAL OF MEDICINAL CHEMISTRY (2012)
Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles
Iana M. Serafimova et al.
NATURE CHEMICAL BIOLOGY (2012)
Mutations in UVSSA cause UV-sensitive syndrome and destabilize ERCC6 in transcription-coupled DNA repair
Xue Zhang et al.
NATURE GENETICS (2012)
AXL and acquired resistance to EGFR inhibitors
Sophie Postel-Vinay et al.
NATURE GENETICS (2012)
Drug repositioning for Alzheimer's disease
Anne Corbett et al.
NATURE REVIEWS DRUG DISCOVERY (2012)
Ranibizumab Combined With Low-Dose Sorafenib for Exudative Age-Related Macular Degeneration
Teresa Diago et al.
MAYO CLINIC PROCEEDINGS (2012)
Mechanisms of Age-Related Macular Degeneration
Jayakrishna Ambati et al.
NEURON (2012)
Placebo-Controlled Trial of Tofacitinib Monotherapy in Rheumatoid Arthritis
Roy Fleischmann et al.
NEW ENGLAND JOURNAL OF MEDICINE (2012)
Safety and Activity of Anti-PD-L1 Antibody in Patients with Advanced Cancer
Julie R. Brahmer et al.
NEW ENGLAND JOURNAL OF MEDICINE (2012)
Conjugate Adaptation of Smooth Pursuit during Monocular Viewing in Strabismic Monkeys with Exotropia
Seiji Ono et al.
INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE (2012)
Combining immunotherapy and targeted therapies in cancer treatment
Matthew Vanneman et al.
NATURE REVIEWS CANCER (2012)
Redox-Based Probes for Protein Tyrosine Phosphatases
Stephen E. Leonard et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2011)
Receptor Tyrosine Kinases and Targeted Cancer Therapeutics
Kenji Takeuchi et al.
BIOLOGICAL & PHARMACEUTICAL BULLETIN (2011)
Receptor Tyrosine Kinases and TLR/IL1 Rs Unexpectedly Activate Myeloid Cell PI3Kγ, A Single Convergent Point Promoting Tumor Inflammation and Progression
Michael C. Schmid et al.
CANCER CELL (2011)
Hallmarks of Cancer: The Next Generation
Douglas Hanahan et al.
CELL (2011)
In Situ Kinase Profiling Reveals Functionally Relevant Properties of Native Kinases
Matthew P. Patricelli et al.
CHEMISTRY & BIOLOGY (2011)
High-Throughput Kinase Profiling: A More Efficient Approach toward the Discovery of New Kinase Inhibitors
Chandrasekhar V. Miduturu et al.
CHEMISTRY & BIOLOGY (2011)
New Frontiers in Chemical Biology: Enabling Drug Discovery. Edited by Mark E. Bunnage.
Joshua Kritzer
ChemMedChem (2011)
Signaling cell death from the endoplasmic reticulum stress response
Gordon C. Shore et al.
CURRENT OPINION IN CELL BIOLOGY (2011)
Mechanisms of drug resistance in kinases
Rina Barouch-Bentov et al.
EXPERT OPINION ON INVESTIGATIONAL DRUGS (2011)
Role of LRRK2 kinase dysfunction in Parkinson disease
Azad Kumar et al.
EXPERT REVIEWS IN MOLECULAR MEDICINE (2011)
Inhibition of Focal Adhesion Kinase by PF-562,271 Inhibits the Growth and Metastasis of Pancreatic Cancer Concomitant with Altering the Tumor Microenvironment
Jayme B. Stokes et al.
MOLECULAR CANCER THERAPEUTICS (2011)
IC261 induces cell cycle arrest and apoptosis of human cancer cells via CK1δ/ε and Wnt/β-catenin independent inhibition of mitotic spindle formation
J. K. Cheong et al.
ONCOGENE (2011)
Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK
Ryohei Katayama et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2011)
Isoform-specific regulation of Akt by PDGF-induced reactive oxygen species
Revati Wani et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2011)
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
Xianming Deng et al.
ACS MEDICINAL CHEMISTRY LETTERS (2011)
Inhibition of ALK, PI3K/MEK, and HSP90 in Murine Lung Adenocarcinoma Induced by EML4-ALK Fusion Oncogene
Zhao Chen et al.
CANCER RESEARCH (2010)
Understanding Kinase Selectivity Through Energetic Analysis of Binding Site Waters
Daniel D. Robinson et al.
CHEMMEDCHEM (2010)
The (un)targeted cancer kinome
Oleg Fedorov et al.
NATURE CHEMICAL BIOLOGY (2010)
An Oral Spleen Tyrosine Kinase (Syk) Inhibitor for Rheumatoid Arthritis.
Michael E. Weinblatt et al.
NEW ENGLAND JOURNAL OF MEDICINE (2010)
Vinyl sulfone: a versatile function for simple bioconjugation and immobilization
Julia Morales-Sanfrutos et al.
ORGANIC & BIOMOLECULAR CHEMISTRY (2010)
Activity-based protein profiling for biochemical pathway discovery in cancer
Daniel K. Nomura et al.
NATURE REVIEWS CANCER (2010)
Leucine-rich repeat kinase 2 mutations and Parkinson's disease: three questions
Elisa Greggio et al.
ASN NEURO (2009)
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 Ovary
Robin A. Artac et al.
BIOLOGY OF REPRODUCTION (2009)
IRE1α Kinase Activation Modes Control Alternate Endoribonuclease Outputs to Determine Divergent Cell Fates
Dan Han et al.
CELL (2009)
Targeting protein kinases for the development of anti-inflammatory drugs
Philip Cohen
CURRENT OPINION IN CELL BIOLOGY (2009)
Protein kinases as antibacterial targets
Mark Schreiber et al.
CURRENT OPINION IN CELL BIOLOGY (2009)
Targeting cancer with small molecule kinase inhibitors
Jianming Zhang et al.
NATURE REVIEWS CANCER (2009)
An orally bioavailable spleen tyrosine kinase inhibitor delays disease progression and prolongs survival in murine lupus
Frances Rena Bahjat et al.
ARTHRITIS AND RHEUMATISM (2008)
Role of the active-site solvent in the thermodynamics of factor Xa ligand binding
Robert Abel et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2008)
Phenotype, genotype, and worldwide genetic penetrance of LRRK2-associated Parkinson's disease: a case-control study
Daniel G. Healy et al.
LANCET NEUROLOGY (2008)
High-throughput kinase profiling as a platform for drug discovery
David M. Goldstein et al.
NATURE REVIEWS DRUG DISCOVERY (2008)
Immunobiology of the TAM receptors
Greg Lemke et al.
NATURE REVIEWS IMMUNOLOGY (2008)
Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors
Marcus Bantscheff et al.
NATURE BIOTECHNOLOGY (2007)
Macrophages and dendritic cells use different Axl/Mertk/Tyro3 receptors in clearance of apoptotic cells
Heather M. Seitz et al.
JOURNAL OF IMMUNOLOGY (2007)
Motifs for molecular recognition exploiting hydrophobic enclosure in protein-ligand binding
Tom Young et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2007)
PI3K delta and PI3K gamma: partners in crime in inflammation in rheumatoid arthritis and beyond?
Christian Rommel et al.
NATURE REVIEWS IMMUNOLOGY (2007)
The crystal structure of human IRE1 luminal domain reveals a conserved dimerization interface required for activation of the unfolded protein response
Jiahai Zhou et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2006)
Natural killer cell differentiation driven by Tyro3 receptor tyrosine kinases
Anouk Caraux et al.
NATURE IMMUNOLOGY (2006)
Elevated growth-arrest-specific protein 6 plasma levels in patients with severe sepsis
D Borgel et al.
CRITICAL CARE MEDICINE (2006)
Toll-Like Receptor (TLR) Response Tolerance: A Key Physiological Damage Limitation Effect and an Important Potential Opportunity for Therapy
Andrea Broad et al.
CURRENT MEDICINAL CHEMISTRY (2006)
On the mechanism of sensing unfolded protein in the endoplasmic reticulum
JJ Credle et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2005)
Cancer regression and autoimmunity induced by cytotoxic T lymphocyte-associated antigen 4 blockade in patients with metastatic melanoma
GQ Phan et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2003)
Thermodynamic contributions of the ordered water molecule in HIV-1 protease
Z Li et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2003)
Protein kinase inhibitors as a therapeutic modality
A Levitzki
ACCOUNTS OF CHEMICAL RESEARCH (2003)
An integrated stress response regulates amino acid metabolism and resistance to oxidative stress
HP Harding et al.
MOLECULAR CELL (2003)
The protein kinase complement of the human genome
G Manning et al.
SCIENCE (2002)
IRE1 couples endoplasmic reticulum load to secretory capacity by processing the XBP-1 mRNA
M Calfon et al.
NATURE (2002)
Phosphoproteome analysis by mass spectrometry and its application to Saccharomyces cerevisiae
SB Ficarro et al.
NATURE BIOTECHNOLOGY (2002)
XBP1 mRNA is induced by ATF6 and spliced by IRE1 in response to ER stress to produce a highly active transcription factor
H Yoshida et al.
CELL (2001)
The regulation of protein function by multisite phosphorylation - a 25 year update
P Cohen
TRENDS IN BIOCHEMICAL SCIENCES (2000)