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KRAS is vulnerable to reversible switch-II pocket engagement in cells
Current small-molecule inhibitors of KRAS(G12C) bind irreversibly in the switch-II pocket (SII-P), exploiting the strong nucleophilicity of the acquired cysteine as well as the preponderance of the GDP-bound form of this mutant. Nevertheless, many oncogenic KRAS mutants lack these two features, and...
Autores principales: | Vasta, James D., Peacock, D. Matthew, Zheng, Qinheng, Walker, Joel A., Zhang, Ziyang, Zimprich, Chad A., Thomas, Morgan R., Beck, Michael T., Binkowski, Brock F., Corona, Cesear R., Robers, Matthew B., Shokat, Kevan M. |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Nature Publishing Group US
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9135634/ https://www.ncbi.nlm.nih.gov/pubmed/35314814 http://dx.doi.org/10.1038/s41589-022-00985-w |
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