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

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 d...

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Pubblicato in:Science
Autori principali: Lito, Piro, Solomon, Martha, Li, Lian-Sheng, Hansen, Rasmus, Rosen, Neal
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2016
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Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC4955282/
https://ncbi.nlm.nih.gov/pubmed/26841430
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1126/science.aad6204
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