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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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| Veröffentlicht in: | Science |
|---|---|
| Hauptverfasser: | , , , , |
| Format: | Artigo |
| Sprache: | Inglês |
| Veröffentlicht: |
2016
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| Schlagworte: | |
| Online Zugang: | 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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