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...

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Detalles Bibliográficos
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.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group US 2022
Materias:
Article
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

Internet

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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