Chemoselective Covalent Modification of K-Ras(G12R) with a Small Molecule Electrophile

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

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

KRAS is vulnerable to reversible switch-II pocket engagement in cells

(2022) James D. Vasta et al.   Nature Chemical Biology

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

RAS-targeted therapies: is the undruggable drugged?

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

Reversible histone glycation is associated with disease-related changes in chromatin architecture

(2019) Qingfei Zheng et al.   Nature Communications

KRASG12C inhibition produces a driver-limited state revealing collateral dependencies

(2019) Kevin Lou et al.   Science Signaling

Improving mass spectrometry analysis of protein structures with arginine-selective chemical cross-linkers

(2019) Alexander X. Jones et al.   Nature Communications

Atypical KRASG12R Mutant Is Impaired in PI3K Signaling and Macropinocytosis in Pancreatic Cancer

(2019) G. Aaron Hobbs 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

Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor

(2018) Matthew R. Janes et al.   CELL

The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors

(2018) Rasmus Hansen et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Arginine-selective bioconjugation with 4-azidophenyl glyoxal: application to the single and dual functionalisation of native antibodies

(2018) Igor Dovgan et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors

(2018) Rasmus Hansen et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Methylglyoxal-derived posttranslational arginine modifications are abundant histone marks

(2018) James J. Galligan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Arginine selective reagents for ligation to peptides and proteins

(2016) Darren A. Thompson et al.   JOURNAL OF PEPTIDE SCIENCE

Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design

(2016) Jonathan M. L. Ostrem et al.   NATURE REVIEWS DRUG DISCOVERY

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

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

Biochemical and Structural Analysis of Common Cancer-Associated KRAS Mutations

(2015) J. C. Hunter et al.   MOLECULAR CANCER RESEARCH

Arginine Modifications by Methylglyoxal: Discovery in a Recombinant Monoclonal Antibody and Contribution to Acidic Species

(2013) Chris Chumsae et al.   ANALYTICAL CHEMISTRY

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

(2013) Jonathan M. Ostrem et al.   NATURE

Arginine-Specific Modification of Proteins with Polyethylene Glycol

(2010) Marc A. Gauthier et al.   BIOMACROMOLECULES

Reaction of the Butter Flavorant Diacetyl (2,3-Butanedione) withN-α-Acetylarginine: A Model for Epitope Formation with Pulmonary Proteins in the Etiology of Obliterative Bronchiolitis

(2010) James M. Mathews et al.   JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY