Enhanced Suppression of a Protein–Protein Interaction in Cells Using Small-Molecule Covalent Inhibitors Based on an N-Acyl-N-alkyl Sulfonamide Warhead

Ligand Conformational Bias Drives Enantioselective Modification of a Surface-Exposed Lysine on Hsp90

(2020) Adolfo Cuesta et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

MIRROS: a randomized, placebo-controlled, Phase III trial of cytarabine ± idasanutlin in relapsed or refractory acute myeloid leukemia

(2020) Pau Montesinos et al.   Future Oncology

Bicyclobutane Carboxylic Amide as a Cysteine-Directed Strained Electrophile for Selective Targeting of Proteins

(2020) Keisuke Tokunaga et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Site-specific covalent labeling of His-tag fused proteins with N-acyl-N-alkyl sulfonamide reagent

(2020) Vikram Thimaradka et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Selective and reversible modification of kinase cysteines with chlorofluoroacetamides

(2019) Naoya Shindo et al.   Nature Chemical Biology

Covalent Inhibitors of Protein–Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues

(2019) Luca Gambini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of a Cell-Based Ligand-Screening System for Identifying Hsp90 Inhibitors

(2019) Tsuyoshi Ueda et al.   BIOCHEMISTRY

Global targeting of functional tyrosines using sulfur-triazole exchange chemistry

(2019) Heung Sik Hahm et al.   Nature Chemical Biology

Structure-based design of targeted covalent inhibitors

(2018) Richard Lonsdale et al.   CHEMICAL SOCIETY REVIEWS

Rapid labelling and covalent inhibition of intracellular native proteins using ligand-directed N-acyl-N-alkyl sulfonamide

(2018) Tomonori Tamura et al.   Nature Communications

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

Chemistry for Covalent Modification of Endogenous/Native Proteins: From Test Tubes to Complex Biological Systems

(2018) Tomonori Tamura et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

“Inverse Drug Discovery” Strategy To Identify Proteins That Are Targeted by Latent Electrophiles As Exemplified by Aryl Fluorosulfates

(2017) David E. Mortenson et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeting the N terminus for site-selective protein modification

(2017) Christian B Rosen et al.   Nature Chemical Biology

Targeted Covalent Inhibitors for Drug Design

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

Proximity-enabled bioreactivity to generate covalent peptide inhibitors of p53–Mdm4

(2016) Christian Hoppmann et al.   CHEMICAL COMMUNICATIONS

Arylfluorosulfates Inactivate Intracellular Lipid Binding Protein(s) through Chemoselective SuFEx Reaction with a Binding Site Tyr Residue

(2016) Wentao Chen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

jPOSTrepo: an international standard data repository for proteomes

(2016) Shujiro Okuda et al.   NUCLEIC ACIDS RESEARCH

Acquired EGFR C797S mutation mediates resistance to AZD9291 in non–small cell lung cancer harboring EGFR T790M

(2015) Kenneth S Thress et al.   NATURE MEDICINE

Small-Molecule Inhibitors of Protein-Protein Interactions: Progressing toward the Reality

(2014) Michelle R. Arkin et al.   CHEMISTRY & BIOLOGY

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

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

Drugging the p53 pathway: understanding the route to clinical efficacy

(2014) Kian Hoe Khoo et al.   NATURE REVIEWS DRUG DISCOVERY

MDM2 Small-Molecule Antagonist RG7112 Activates p53 Signaling and Regresses Human Tumors in Preclinical Cancer Models

(2013) C. Tovar et al.   CANCER RESEARCH

Synthesis of γ-labeled nucleoside 5′-triphosphates using click chemistry

(2013) S. Serdjukow et al.   CHEMICAL COMMUNICATIONS

Discovery of RG7388, a Potent and Selective p53–MDM2 Inhibitor in Clinical Development

(2013) Qingjie Ding et al.   JOURNAL OF MEDICINAL CHEMISTRY

Differential regulation of p21waf1protein half-life by DNA damage and Nutlin-3 in p53 wild-type tumors and its therapeutic implications

(2012) Li-Ju Chang et al.   CANCER BIOLOGY & THERAPY

Ordering of the N-Terminus of Human MDM2 by Small Molecule Inhibitors

(2012) Klaus Michelsen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Protein-protein docking benchmark version 4.0

(2010) Howook Hwang et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

Oligobenzamide proteomimetic inhibitors of the p53–hDM2 protein–protein interaction

(2009) Jeffrey P. Plante et al.   CHEMICAL COMMUNICATIONS

Structural basis for high-affinity peptide inhibition of p53 interactions with MDM2 and MDMX

(2009) M. Pazgier et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA