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Chemoselective Covalent Modification of K-Ras(G12R) with a Small Molecule Electrophile

[Image: see text] KRAS mutations are one of the most common oncogenic drivers in human cancer. While small molecule inhibitors for the G12C mutant have been successfully developed, allele-specific inhibition for other KRAS hotspot mutants remains challenging. Here we report the discovery of covalent...

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Detalles Bibliográficos
Autores principales: Zhang, Ziyang, Morstein, Johannes, Ecker, Andrew K., Guiley, Keelan Z., Shokat, Kevan M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9460778/
https://www.ncbi.nlm.nih.gov/pubmed/36001446
http://dx.doi.org/10.1021/jacs.2c05377