Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor

High-Throughput Kinetic Characterization of Irreversible Covalent Inhibitors of KRASG12C by Intact Protein MS and Targeted MRM

(2022) Ke Sherry Li et al.   ANALYTICAL CHEMISTRY

The path to the clinic: a comprehensive review on direct KRASG12C inhibitors

(2022) Albert K. Kwan et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Conformation-locking antibodies for the discovery and characterization of KRAS inhibitors

(2022) Christopher W. Davies et al.   NATURE BIOTECHNOLOGY

Expanding the Reach of Precision Oncology by Drugging All KRAS Mutants

(2022) Marco H. Hofmann et al.   Cancer Discovery

Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor

(2021) Xiaolun Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Frequency of Ras Mutations in Cancer

(2020) Ian A. Prior et al.   CANCER RESEARCH

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

Drugging all RAS isoforms with one pocket

(2020) Dirk Kessler et al.   Future Medicinal Chemistry

RAS-targeted therapies: is the undruggable drugged?

(2020) Amanda R. Moore et al.   NATURE REVIEWS DRUG DISCOVERY

BI-3406, a potent and selective SOS1::KRAS interaction inhibitor, is effective in KRAS-driven cancers through combined MEK inhibition

(2020) Marco H Hofmann et al.   Cancer Discovery

Drugging an undruggable pocket on KRAS

(2019) Dirk Kessler et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Expanding the Armory: Predicting and Tuning Covalent Warhead Reactivity

(2017) Richard Lonsdale et al.   Journal of Chemical Information and Modeling

Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism

(2016) P. Lito et al.   SCIENCE

Intrinsic reactivity profile of electrophilic moieties to guide covalent drug design: N-α-acetyl-l-lysine as an amine nucleophile

(2016) Upendra P. Dahal et al.   MedChemComm

Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State

(2016) M. P. Patricelli et al.   Cancer Discovery

A method for the second-site screening of K-Ras in the presence of a covalently attached first-site ligand

(2014) Qi Sun et al.   JOURNAL OF BIOMOLECULAR NMR

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

(2013) Jonathan M. Ostrem et al.   NATURE

Using chemical shift perturbation to characterise ligand binding

(2013) Mike P. Williamson   PROGRESS IN NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY

Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation

(2012) Qi Sun et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity

(2012) T. Maurer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA