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Article

Ras Binder Induces a Modified Switch-II Pocket in GTP and GDP States.

Cell chemical biology - 21 Dec 2017

Gentile Daniel R, Rathinaswamy Manoj K, Jenkins Meredith L, Moss Steven M, Siempelkamp Braden D, Renslo Adam R, Burke John E, Shokat Kevan M

Abstract excerpt

Covalent inhibitors of K-Ras(G12C) have been reported that exclusively recognize the GDP state. Here, we utilize disulfide tethering of a non-natural cysteine (K-Ras(M72C)) to identify a new switch-II pocket (S-IIP) binding ligand (2C07) that engages the active GTP state. Co-crystal structures of 2C07 bound to H-Ras(M72C) reveal binding in a cryptic groove we term S-IIG. In the GppNHp state, 2C07 binding to a...

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Identifiers

PMID: 29033317
DOI: 10.1016/j.chembiol.2017.08.025
PMCID: PMC5915340

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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