Selective and reversible modification of kinase cysteines with chlorofluoroacetamides

Targeted Covalent Inhibitors for Drug Design

(2016) Thomas A. Baillie   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Breast Cancer Resistance to Antiestrogens Is Enhanced by Increased ER Degradation and ERBB2 Expression

(2016) Tomohiro Shibata et al.   CANCER RESEARCH

Targeting biomolecules with reversible covalent chemistry

(2016) Anupam Bandyopadhyay et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Using Protein-Confined Proximity To Determine Chemical Reactivity

(2016) Tomonori Kobayashi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Proteome-wide covalent ligand discovery in native biological systems

(2016) Keriann M. Backus et al.   NATURE

Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors

(2016) Tinghu Zhang et al.   Nature Chemical Biology

Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain

(2016) Gizem Akçay et al.   Nature Chemical Biology

Phosphorylation of mTOR Ser2481 is a key target limiting the efficacy of rapalogs for treating hepatocellular carcinoma

(2016) Kosuke Watari et al.   Oncotarget

Systematic Study of the Glutathione (GSH) Reactivity of N-Arylacrylamides: 1. Effects of Aryl Substitution

(2015) Victor J. Cee et al.   JOURNAL OF MEDICINAL CHEMISTRY

Prolonged and tunable residence time using reversible covalent kinase inhibitors

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

Tricyclic Covalent Inhibitors Selectively Target Jak3 through an Active Site Thiol

(2015) Eric R. Goedken et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

Chemical and Computational Methods for the Characterization of Covalent Reactive Groups for the Prospective Design of Irreversible Inhibitors

(2014) Mark E. Flanagan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Promiscuity and Selectivity in Covalent Enzyme Inhibition: A Systematic Study of Electrophilic Fragments

(2014) Christian Jöst et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer

(2014) D. A. E. Cross et al.   Cancer Discovery

Benchmarking in Vitro Covalent Binding Burden As a Tool To Assess Potential Toxicity Caused by Nonspecific Covalent Binding of Covalent Drugs

(2013) Upendra P. Dahal et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

Discovery of a Potent and Isoform-Selective Targeted Covalent Inhibitor of the Lipid Kinase PI3Kα

(2013) Mariana Nacht et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Towards automated crystallographic structure refinement withphenix.refine

(2012) Pavel V. Afonine et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Irreversible Protein Kinase Inhibitors: Balancing the Benefits and Risks

(2012) Tjeerd Barf et al.   JOURNAL OF MEDICINAL CHEMISTRY

Iminoboronates: A New Strategy for Reversible Protein Modification

(2012) Pedro M. S. D. Cal et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles

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

Structural basis for the altered drug sensitivities of non-small cell lung cancer-associated mutants of human epidermal growth factor receptor

(2012) S Yoshikawa et al.   ONCOGENE

Structure-Based Approach for the Discovery of Pyrrolo[3,2-d]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors

(2012) Satoshi Sogabe et al.   ACS Medicinal Chemistry Letters

LigPlot+: Multiple Ligand–Protein Interaction Diagrams for Drug Discovery

(2011) Roman A. Laskowski et al.   Journal of Chemical Information and Modeling

The resurgence of covalent drugs

(2011) Juswinder Singh et al.   NATURE REVIEWS DRUG DISCOVERY

Targeted covalent drugs of the kinase family

(2010) Juswinder Singh et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Strategies for discovering and derisking covalent, irreversible enzyme inhibitors

(2010) Douglas S Johnson et al.   Future Medicinal Chemistry

Selective Covalent Labeling of Tag-Fused GPCR Proteins on Live Cell Surface with a Synthetic Probe for Their Functional Analysis

(2010) Hiroshi Nonaka et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Quantitative reactivity profiling predicts functional cysteines in proteomes

(2010) Eranthie Weerapana et al.   NATURE

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

Covalent Modifiers: An Orthogonal Approach to Drug Design

(2009) Michele H. Potashman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Activity-Based Protein Profiling: From Enzyme Chemistry to Proteomic Chemistry

(2008) Benjamin F. Cravatt et al.   Annual Review of Biochemistry

BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models

(2008) D Li et al.   ONCOGENE