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Article

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

Science (New York, N.Y.) - 5 Feb 2016

Lito Piro, Solomon Martha, Li Lian-Sheng, Hansen Rasmus, Rosen Neal

Abstract excerpt

It is thought that KRAS oncoproteins are constitutively active because their guanosine triphosphatase (GTPase) activity is disabled. Consequently, drugs targeting the inactive or guanosine 5'-diphosphate-bound conformation are not expected to be effective. We describe a mechanism that enables such drugs to inhibit KRAS(G12C) signaling and cancer cell growth. Inhibition requires intact GTPase activity and occurs...

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Source

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Identifiers

PMID: 26841430
DOI: 10.1126/science.aad6204
PMCID: PMC4955282

Genes

KRAS

Variants

Provenance

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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Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism.PMID 26841430Read ↗

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