Related references
Note: Only part of the references are listed.Discovery of Non-Cysteine-Targeting Covalent Inhibitors by Activity-Based Proteomic Screening with a Cysteine-Reactive Probe
Yejin Jung et al.
ACS CHEMICAL BIOLOGY (2022)
Efficient targeted oncogenic KRASG12C degradation via first reversible-covalent PROTAC
Fang Yang et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)
Recent applications of vinyl sulfone motif in drug design and discovery
Reza Ahmadi et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)
Epoxides: Developability as active pharmaceutical ingredients and biochemical probes
Baljit Kaur et al.
BIOORGANIC CHEMISTRY (2022)
Approaches to mitigate the risk of serious adverse reactions in covalent drug design
Thomas A. Baillie
EXPERT OPINION ON DRUG DISCOVERY (2021)
Discovery of 4,4′-Dipyridylsulfide Analogs as Switchable Electrophiles for Covalent Inhibition
Yeong-Chan Ahn et al.
ACS CHEMICAL BIOLOGY (2021)
Characterization of an aromatic trifluoromethyl ketone as a new warhead for covalently reversible kinase inhibitor design
Zhen Zhang et al.
BIOORGANIC & MEDICINAL CHEMISTRY (2021)
Recent progress in covalent warheads for in vivo targeting of endogenous proteins
Naoya Shindo et al.
BIOORGANIC & MEDICINAL CHEMISTRY (2021)
Novel Electrophilic Warhead Targeting a Triple-Negative Breast Cancer Driver in Live Cells Revealed by Inverse Drug Discovery
Youlong Fan et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
Strategic Design of Catalytic Lysine-Targeting Reversible Covalent BCR-ABL Inhibitors
David Quach et al.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)
Covalent Small Molecule Immunomodulators Targeting the Protease Active Site
Hong-Rae Kim et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo
Christian Dubiella et al.
NATURE CHEMICAL BIOLOGY (2021)
Clinical Acquired Resistance to KRASG12C Inhibition through a novel KRAS Switch-II Pocket Mutation and Polyclonal Alterations Converging on RAS-MAPK Reactivation
Noritaka Tanaka et al.
CANCER DISCOVERY (2021)
Recent advances in the development of covalent inhibitors
Hyunsoo Kim et al.
RSC MEDICINAL CHEMISTRY (2021)
Fragment-based covalent ligand discovery
Wenchao Lu et al.
RSC CHEMICAL BIOLOGY (2021)
Ubiquitin C-Terminal Hydrolase L1: Biochemical and Cellular Characterization of a Covalent Cyanopyrrolidine-Based Inhibitor
Aaron D. Krabill et al.
CHEMBIOCHEM (2020)
Cyanopyrrolidine Inhibitors of Ubiquitin Specific Protease 7 Mediate Desulfhydration of the Active-Site Cysteine
Charlene Bashore et al.
ACS CHEMICAL BIOLOGY (2020)
Epoxide containing molecules: A good or a bad drug design approach
Ana R. Gomes et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)
Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease
Wenhao Dai et al.
SCIENCE (2020)
Selective Covalent Targeting of Mutated EGFR(T790M) with Chlorofluoroacetamide-Pyrimidines
Mami Sato et al.
ACS MEDICINAL CHEMISTRY LETTERS (2020)
2-Sulfonylpyridines as Tunable, Cysteine-Reactive Electrophiles
Claudio Zambaldo et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2020)
Alkynyl Benzoxazines and Dihydroquinazolines as Cysteine Targeting Covalent Warheads and Their Application in Identification of Selective Irreversible Kinase Inhibitors
Kirsten McAulay et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2020)
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4
Robin A. Fairhurst et al.
JOURNAL OF MEDICINAL CHEMISTRY (2020)
Bicyclobutane Carboxylic Amide as a Cysteine-Directed Strained Electrophile for Selective Targeting of Proteins
Keisuke Tokunaga et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2020)
Covalent inhibition of NSD1 histone methyltransferase
Huang Huang et al.
NATURE CHEMICAL BIOLOGY (2020)
Crystallographic and electrophilic fragment screening of the SARS-CoV-2 main protease
Alice Douangamath et al.
NATURE COMMUNICATIONS (2020)
Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening
Efrat Resnick et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2019)
Structural basis for the inhibitory effects of a novel reversible covalent ligand on PPARγ phosphorylation
Jun Young Jang et al.
SCIENTIFIC REPORTS (2019)
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology
Matthias Gehringer et al.
JOURNAL OF MEDICINAL CHEMISTRY (2019)
Selective and reversible modification of kinase cysteines with chlorofluoroacetamides
Naoya Shindo et al.
NATURE CHEMICAL BIOLOGY (2019)
DrugBank 5.0: a major update to the DrugBank database for 2018
David S. Wishart et al.
NUCLEIC ACIDS RESEARCH (2018)
Intravenous Fosfomycin: An Assessment of Its Potential for Use in the Treatment of Systemic Infections in Canada
George G. Zhanel et al.
CANADIAN JOURNAL OF INFECTIOUS DISEASES & MEDICAL MICROBIOLOGY (2018)
Targeting STING with covalent small-molecule inhibitors
Simone M. Haag et al.
NATURE (2018)
A road map for prioritizing warheads for cysteine targeting covalent inhibitors
Peter Abranyi-Balogh et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)
Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions
Paul A. Jackson et al.
JOURNAL OF MEDICINAL CHEMISTRY (2017)
Covalent inhibitors design and discovery
Stephane De Cesco et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2017)
Determining Cysteines Available for Covalent Inhibition Across the Human Kinome
Zheng Zhao et al.
JOURNAL OF MEDICINAL CHEMISTRY (2017)
Strain-Release Heteroatom Functionalization: Development, Scope, and Stereospecificity
Justin M. Lopchuk et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2017)
Ability of Bruton's Tyrosine Kinase Inhibitors to Sequester Y551 and Prevent Phosphorylation Determines Potency for Inhibition of Fc Receptor but not B-Cell Receptor Signaling
Andrew T. Bender et al.
MOLECULAR PHARMACOLOGY (2017)
Fosfomycin: Pharmacological, Clinical and Future Perspectives
Anneke Corinne Dijkmans et al.
ANTIBIOTICS-BASEL (2017)
Development of 5N-Bicalutamide, a High-Affinity Reversible Covalent Antiandrogen
Felipe de Jesus Cortez et al.
ACS CHEMICAL BIOLOGY (2017)
2-Chloropropionamide As a Low-Reactivity Electrophile for Irreversible Small-Molecule Probe Identification
Dharmaraja Allimuthu et al.
ACS CHEMICAL BIOLOGY (2017)
Covalent Enzyme Inhibition through Fluorosulfate Modification of a Noncatalytic Serine Residue
Olugbeminiyi O. Fadeyi et al.
ACS CHEMICAL BIOLOGY (2017)
Covalent Protein Labeling at Glutamic Acids
Pablo Martin-Gago et al.
CELL CHEMICAL BIOLOGY (2017)
Chemoproteomic Screening of Covalent Ligands Reveals UBA5 As a Novel Pancreatic Cancer Target
Allison M. Roberts et al.
ACS CHEMICAL BIOLOGY (2017)
Targeting biomolecules with reversible covalent chemistry
Anupam Bandyopadhyay et al.
CURRENT OPINION IN CHEMICAL BIOLOGY (2016)
Covalent targeting of acquired cysteines in cancer
Marieke Visscher et al.
CURRENT OPINION IN CHEMICAL BIOLOGY (2016)
Synthetic Aziridines in Medicinal Chemistry: A Mini-Review
Girija S. Singh
MINI-REVIEWS IN MEDICINAL CHEMISTRY (2016)
Quantifying tetrahedral adduct formation and stabilization in the cysteine and the serine proteases
Jennifer A. Cleary et al.
BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS (2015)
Covalent inhibitors in drug discovery: from accidental discoveries to avoided liabilities and designed therapies
Renato A. Bauer
DRUG DISCOVERY TODAY (2015)
Evaluation of trypanocidal activity of combinations of anti-sleeping sickness drugs with cysteine protease inhibitors
Dietmar Steverding
EXPERIMENTAL PARASITOLOGY (2015)
Prolonged and tunable residence time using reversible covalent kinase inhibitors
J. Michael Bradshaw et al.
NATURE CHEMICAL BIOLOGY (2015)
Cysteine proteases as therapeutic targets: does selectivity matter? A systematic review of calpain and cathepsin inhibitors
Marton Siklos et al.
ACTA PHARMACEUTICA SINICA B (2015)
Modeling the Clinical Phenotype of BTK Inhibition in the Mature Murine Immune System
Micah J. Benson et al.
JOURNAL OF IMMUNOLOGY (2014)
Targeting transcription regulation in cancer with a covalent CDK7 inhibitor
Nicholas Kwiatkowski et al.
NATURE (2014)
Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors
Li Tan et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2014)
Diverse Functional Roles of Reactive Cysteines
Nicholas J. Pace et al.
ACS CHEMICAL BIOLOGY (2013)
Chemical Proteomics with Sulfonyl Fluoride Probes Reveals Selective Labeling of Functional Tyrosines in Glutathione Transferases
Christian Gu et al.
CHEMISTRY & BIOLOGY (2013)
Developing Irreversible Inhibitors of the Protein Kinase Cysteinome
Qingsong Liu et al.
CHEMISTRY & BIOLOGY (2013)
An androgen receptor N-terminal domain antagonist for treating prostate cancer
Jae-Kyung Myung et al.
JOURNAL OF CLINICAL INVESTIGATION (2013)
Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors
Rand M. Miller et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2013)
MALT1 Small Molecule Inhibitors Specifically Suppress ABC-DLBCL In Vitro and In Vivo
Lorena Fontan et al.
CANCER CELL (2012)
Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles
Iana M. Serafimova et al.
NATURE CHEMICAL BIOLOGY (2012)
Cysteine Mapping in Conformationally Distinct Kinase Nucleotide Binding Sites: Application to the Design of Selective Covalent Inhibitors
Emeline Leproult et al.
JOURNAL OF MEDICINAL CHEMISTRY (2011)
Regression of Castrate-Recurrent Prostate Cancer by a Small-Molecule Inhibitor of the Amino-Terminus Domain of the Androgen Receptor
Raymond J. Andersen et al.
CANCER CELL (2010)
Targeting cancer with small molecule kinase inhibitors
Jianming Zhang et al.
NATURE REVIEWS CANCER (2009)
Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR
Anja Michalczyk et al.
BIOORGANIC & MEDICINAL CHEMISTRY (2008)
Idiosyncratic drug reactions: Past, present, and future
Jack Uetrecht
CHEMICAL RESEARCH IN TOXICOLOGY (2008)
A cysteine protease inhibitor cures Chagas' disease in an immunodeficient-mouse model of infection
Patricia S. Doyle et al.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY (2007)
Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib
EL Kwak et al.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2005)
Evidence that the fosfomycin target Cys115 in UDP-N-acetylglucosamine enolpyruvyl transferase (MurA) is essential for product release
S Eschenburg et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2005)
Irreversible inhibitors of serine, cysteine, and threonine proteases
JC Powers et al.
CHEMICAL REVIEWS (2002)
Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662
LM Leesnitzer et al.
BIOCHEMISTRY (2002)