Associated Papers
Systematic cysteine scanning identifies a druggable pocket in oncogenic KRAS.
van Tienen LM et al.
Cell Chemical Biology, 2026
Mechanistic insights into KRASG12D inhibitor binding revealed by molecular dynamics simulations of multiple crystal structures.
Kim D et al.
Physical Chemistry Chemical Physics : Pccp, 2026
Distal Covalent Targeting Suppresses Signaling of Oncogenic K-Ras(G13C) in Cancer Cells.
Zheng Q et al.
Acs Chemical Biology, 2025
Denitrogenative Alkylation of K-Ras(G12D) Inhibits Oncogenic Signaling in Cancer Cells.
Zheng Q et al.
Journal of the American Chemical Society, 2025
Biophysical and structural analysis of KRAS switch-II pocket inhibitors reveals allele-specific binding constraints.
Alexander P et al.
The Journal of Biological Chemistry, 2025
The structure of KRASG12C bound to divarasib highlights features of potent switch-II pocket engagement.
Fernando MC et al.
Small Gtpases, 2024
Comprehensive structure-function analysis reveals gain- and loss-of-function mechanisms impacting oncogenic KRAS activity.
Kwon JJ et al.
Biorxiv : the Preprint Server for Biology, 2024
Strain-release alkylation of Asp12 enables mutant selective targeting of K-Ras-G12D.
Zheng Q et al.
Nature Chemical Biology, 2024
Discovery of MK-1084: An Orally Bioavailable and Low-Dose KRASG12C Inhibitor.
Ma X et al.
Journal of Medicinal Chemistry, 2024
Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers.
Jiang J et al.
Cancer Discovery, 2024
Exploring switch II pocket conformation of KRAS(G12D) with mutant-selective monobody inhibitors.
Akkapeddi P et al.
Proceedings of the National Academy of Sciences of the United States of America, 2023
Targeting oncogenic KRasG13C with nucleotide-based covalent inhibitors.
Goebel L et al.
Elife, 2023
Chemical acylation of an acquired serine suppresses oncogenic signaling of K-Ras(G12S).
Zhang Z et al.
Nature Chemical Biology, 2022
Chemoselective Covalent Modification of K-Ras(G12R) with a Small Molecule Electrophile.
Zhang Z et al.
Journal of the American Chemical Society, 2022
Oncogenic KRAS G12C: Kinetic and redox characterization of covalent inhibition.
Huynh MV et al.
The Journal of Biological Chemistry, 2022
Delineating the RAS Conformational Landscape.
Parker MI et al.
Cancer Research, 2022
Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C.
Weiss A et al.
Cancer Discovery, 2022
Blockade of mutant RAS oncogenic signaling with a special emphasis on KRAS.
Roskoski R
Pharmacological Research, 2021
Computationally Empowered Workflow Identifies Novel Covalent Allosteric Binders for KRASG12C.
Mortier J et al.
Chemmedchem, 2020
Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State.
Patricelli MP et al.
Cancer Discovery, 2016
K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions.
Ostrem JM et al.
Nature, 2013