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Title
Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors
Authors
Keywords
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Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 65, Issue 1, Pages 58-83
Publisher
American Chemical Society (ACS)
Online
2021-12-29
DOI
10.1021/acs.jmedchem.1c01719
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Note: Only part of the references are listed.- Kinase drug discovery 20 years after imatinib: progress and future directions
- (2021) Philip Cohen et al. NATURE REVIEWS DRUG DISCOVERY
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- (2020) Daniela Angst et al. JOURNAL OF MEDICINAL CHEMISTRY
- Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations
- (2020) Xiaoyun Lu et al. JOURNAL OF MEDICINAL CHEMISTRY
- Alkynyl Benzoxazines and Dihydroquinazolines as Cysteine Targeting Covalent Warheads and Their Application in Identification of Selective Irreversible Kinase Inhibitors
- (2020) Kirsten McAulay et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13
- (2020) Yao Liu et al. JOURNAL OF MEDICINAL CHEMISTRY
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- (2020) Xiao-E Yan et al. JOURNAL OF MEDICINAL CHEMISTRY
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- (2020) Robin A. Fairhurst et al. JOURNAL OF MEDICINAL CHEMISTRY
- TAS-120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure
- (2019) Maria Kalyukina et al. ChemMedChem
- Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton’s Tyrosine Kinase (BTK)
- (2019) Scott H. Watterson et al. JOURNAL OF MEDICINAL CHEMISTRY
- Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations
- (2019) Dennis Bensinger et al. JOURNAL OF MEDICINAL CHEMISTRY
- PF-06651600, a dual JAK3/TEC family kinase inhibitor
- (2019) Hua Xu et al. ACS Chemical Biology
- TAS-120 overcomes resistance to ATP-competitive FGFR inhibitors in patients with FGFR2 fusion-positive intrahepatic cholangiocarcinoma
- (2019) Lipika Goyal et al. Cancer Discovery
- Rotational Freedom, Steric Hindrance, and Protein Dynamics Explain BLU554 Selectivity for the Hinge Cysteine of FGFR4
- (2019) Xiaojing Lin et al. ACS Medicinal Chemistry Letters
- Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase
- (2019) Yunhang Guo et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases
- (2019) Richard D. Caldwell et al. JOURNAL OF MEDICINAL CHEMISTRY
- Design of Potent and Selective Covalent Inhibitors of Bruton’s Tyrosine Kinase Targeting an Inactive Conformation
- (2019) Robert Pulz et al. ACS Medicinal Chemistry Letters
- First-in-Human Phase I Study of Fisogatinib (BLU-554) Validates Aberrant Fibroblast Growth Factor 19 Signaling as a Driver Event in Hepatocellular Carcinoma
- (2019) Richard D Kim et al. Cancer Discovery
- Covalent-Allosteric Inhibitors to Achieve Akt Isoform-Selectivity
- (2019) Lena Quambusch et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- New Promise and Opportunities for Allosteric Kinase Inhibitors
- (2019) Xiaoyun Lu et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Structure-Based Design, Synthesis, and Characterization of the First Irreversible Inhibitor of Focal Adhesion Kinase
- (2018) Expédite Yen-Pon et al. ACS Chemical Biology
- The Cysteinome of Protein Kinases as a Target in Drug Development
- (2018) Apirat Chaikuad et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Structure-based design of targeted covalent inhibitors
- (2018) Richard Lonsdale et al. CHEMICAL SOCIETY REVIEWS
- Improvement in Overall Survival in a Randomized Study That Compared Dacomitinib With Gefitinib in Patients With Advanced Non–Small-Cell Lung Cancer and EGFR-Activating Mutations
- (2018) Tony S. Mok et al. JOURNAL OF CLINICAL ONCOLOGY
- Development, Optimization, and Structure–Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4-d]pyrrolo[2,3-b]pyridine Scaffold
- (2018) Michael Forster et al. JOURNAL OF MEDICINAL CHEMISTRY
- Targeting EGFRL858R/T790M and EGFRL858R/T790M/C797S resistance mutations in NSCLC: Current developments in medicinal chemistry
- (2018) Xiaoyun Lu et al. MEDICINAL RESEARCH REVIEWS
- Dacomitinib: First Global Approval
- (2018) Matt Shirley DRUGS
- Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology
- (2018) Matthias Gehringer et al. JOURNAL OF MEDICINAL CHEMISTRY
- Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects
- (2018) Xiaoyun Lu et al. JOURNAL OF MEDICINAL CHEMISTRY
- Efficacy of a Covalent ERK1/2 Inhibitor, CC-90003, in KRAS-Mutant Cancer Models Reveals Novel Mechanisms of Response and Resistance
- (2018) Ida Aronchik et al. MOLECULAR CANCER RESEARCH
- Fibroblast growth factor receptors as treatment targets in clinical oncology
- (2018) Masaru Katoh Nature Reviews Clinical Oncology
- Determining Cysteines Available for Covalent Inhibition Across the Human Kinome
- (2017) Zheng Zhao et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors
- (2017) Ken A. Brameld et al. JOURNAL OF MEDICINAL CHEMISTRY
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- (2017) Robin A. Fairhurst et al. MedChemComm
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- (2016) Scott H. Watterson et al. JOURNAL OF MEDICINAL CHEMISTRY
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- (2016) W. S. Brown et al. MOLECULAR CANCER THERAPEUTICS
- Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors
- (2016) Tinghu Zhang et al. Nature Chemical Biology
- Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia
- (2016) John C. Byrd et al. NEW ENGLAND JOURNAL OF MEDICINE
- A Perspective on the Kinetics of Covalent and Irreversible Inhibition
- (2016) John M. Strelow SLAS Discovery
- Covalent-Allosteric Kinase Inhibitors
- (2015) Jörn Weisner et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- A phase 1 clinical trial of the selective BTK inhibitor ONO/GS-4059 in relapsed and refractory mature B-cell malignancies
- (2015) H. S. Walter et al. BLOOD
- Development of Selective Covalent Janus Kinase 3 Inhibitors
- (2015) Li Tan et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2
- (2015) Richard A. Ward et al. JOURNAL OF MEDICINAL CHEMISTRY
- Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed
- (2015) Yuliana Yosaatmadja et al. JOURNAL OF STRUCTURAL BIOLOGY
- Prolonged and tunable residence time using reversible covalent kinase inhibitors
- (2015) J Michael Bradshaw et al. Nature Chemical Biology
- First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway
- (2015) M. Hagel et al. Cancer Discovery
- Tricyclic Covalent Inhibitors Selectively Target Jak3 through an Active Site Thiol
- (2015) Eric R. Goedken et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Bruton's tyrosine kinase inhibitors for the treatment of rheumatoid arthritis
- (2014) Jennifer A. Whang et al. DRUG DISCOVERY TODAY
- Ibrutinib: First Global Approval
- (2014) Fiona Cameron et al. DRUGS
- Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor
- (2014) M. Raymond V. Finlay et al. JOURNAL OF MEDICINAL CHEMISTRY
- Targeting transcription regulation in cancer with a covalent CDK7 inhibitor
- (2014) Nicholas Kwiatkowski et al. NATURE
- Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors
- (2014) Li Tan et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer
- (2014) D. A. E. Cross et al. Cancer Discovery
- Developing Irreversible Inhibitors of the Protein Kinase Cysteinome
- (2013) Qingsong Liu et al. CHEMISTRY & BIOLOGY
- Afatinib: First Global Approval
- (2013) Rosselle T. Dungo et al. DRUGS
- Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR)
- (2013) Richard A. Ward et al. JOURNAL OF MEDICINAL CHEMISTRY
- Irreversible Inhibitors of c-Src Kinase That Target a Nonconserved Cysteine
- (2012) Frank E. Kwarcinski et al. ACS Chemical Biology
- The EGFR T790M Mutation in Acquired Resistance to an Irreversible Second-Generation EGFR Inhibitor
- (2012) Y. Kim et al. MOLECULAR CANCER THERAPEUTICS
- Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles
- (2012) Iana M Serafimova et al. Nature Chemical Biology
- Strategies for overcoming resistance to EGFR family tyrosine kinase inhibitors
- (2011) Giuseppe Giaccone et al. CANCER TREATMENT REVIEWS
- New Strategies in Overcoming Acquired Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Lung Cancer
- (2011) G. R. Oxnard et al. CLINICAL CANCER RESEARCH
- Cysteine Mapping in Conformationally Distinct Kinase Nucleotide Binding Sites: Application to the Design of Selective Covalent Inhibitors
- (2011) Emeline Leproult et al. JOURNAL OF MEDICINAL CHEMISTRY
- Chemogenomic Profiling Provides Insights into the Limited Activity of Irreversible EGFR Inhibitors in Tumor Cells Expressing the T790M EGFR Resistance Mutation
- (2010) M. L. Sos et al. CANCER RESEARCH
- A Structure-Guided Approach to Creating Covalent FGFR Inhibitors
- (2010) Wenjun Zhou et al. CHEMISTRY & BIOLOGY
- The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy
- (2010) L. A. Honigberg et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Novel mutant-selective EGFR kinase inhibitors against EGFR T790M
- (2009) Wenjun Zhou et al. NATURE
- Molecular modeling and crystal structure of ERK2–hypothemycin complexes
- (2008) Giulio Rastelli et al. JOURNAL OF STRUCTURAL BIOLOGY
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