JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors

The Ascension of Targeted Covalent Inhibitors

(2022) Juswinder Singh   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C

(2022) Jason G. Kettle et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C

(2022) Andreas Weiss et al.   Cancer Discovery

Adagrasib in Non–Small-Cell Lung Cancer Harboring a KRASG12C Mutation

(2022) Pasi A. Jänne et al.   NEW ENGLAND JOURNAL OF MEDICINE

KRAS secondary mutations that confer acquired resistance to KRAS G12C inhibitors, sotorasib and adagrasib, and overcoming strategies: insights from the in vitro experiments

(2021) Takamasa Koga et al.   Journal of Thoracic Oncology

Clinical acquired resistance to KRASG12C inhibition through a novel KRAS switch-II pocket mutation and polyclonal alterations converging on RAS-MAPK reactivation

(2021) Noritaka Tanaka et al.   Cancer Discovery

KRAS inhibitor-resistance in MET-amplified KRASG12C non-small cell lung cancer induced by RAS- and non-RAS-mediated cell signaling mechanisms

(2021) Shinichiro Suzuki et al.   CLINICAL CANCER RESEARCH

Characterization of KRAS Mutation Subtypes in Non-Small Cell Lung Cancer

(2021) Julia Judd et al.   MOLECULAR CANCER THERAPEUTICS

Sotorasib for Lung Cancers with KRAS p.G12C Mutation

(2021) Ferdinandos Skoulidis et al.   NEW ENGLAND JOURNAL OF MEDICINE

Acquired Resistance to KRASG12C Inhibition in Cancer

(2021) Mark M. Awad et al.   NEW ENGLAND JOURNAL OF MEDICINE

HER2 mediates clinical resistance to the KRASG12C inhibitor sotorasib, which is overcome by co-targeting SHP2

(2021) Cassandra S.L. Ho et al.   EUROPEAN JOURNAL OF CANCER

Diverse alterations associated with resistance to KRAS(G12C) inhibition

(2021) Yulei Zhao et al.   NATURE

Selective KRAS G12C inhibitors in non-small cell lung cancer: chemistry, concurrent pathway alterations, and clinical outcomes

(2021) Gabriela Palma et al.   npj Precision Oncology

Rapid non-uniform adaptation to conformation-specific KRAS(G12C) inhibition

(2020) Jenny Y. Xue et al.   NATURE

Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer

(2020) Jay B. Fell et al.   JOURNAL OF MEDICINAL CHEMISTRY

ReSCoSS: a flexible quantum chemistry workflow identifying relevant solution conformers of drug-like molecules

(2020) Anikó Udvarhelyi et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

KRASG12C Inhibition with Sotorasib in Advanced Solid Tumors

(2020) David S. Hong et al.   NEW ENGLAND JOURNAL OF MEDICINE

The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

(2019) Jude Canon et al.   NATURE

The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients

(2019) Jill Hallin et al.   Cancer Discovery

Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors

(2019) Brian A. Lanman et al.   JOURNAL OF MEDICINAL CHEMISTRY

KRAS: The Critical Driver and Therapeutic Target for Pancreatic Cancer

(2017) Andrew M. Waters et al.   Cold Spring Harbor Perspectives in Medicine

Rapid Determination of the Specificity Constant of Irreversible Inhibitors (kinact/KI) by Means of an Endpoint Competition Assay

(2015) Ikuo Miyahisa et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

Clearance Mechanism Assignment and Total Clearance Prediction in Human Based upon in Silico Models

(2014) Franco Lombardo et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

(2013) Jonathan M. Ostrem et al.   NATURE

Data processing and analysis with theautoPROCtoolbox

(2011) Clemens Vonrhein et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Revealing Atropisomer Axial Chirality in Drug Discovery

(2011) Steven R. LaPlante et al.   ChemMedChem

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Strategies for discovering and derisking covalent, irreversible enzyme inhibitors

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

Ras oncogenes: split personalities

(2008) Antoine E. Karnoub et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY