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KRAS Inhibitor that Simultaneously Inhibits Nucleotide Exchange Activity and Effector Engagement

[Image: see text] We describe a small molecule ligand ACA-14 (2-hydroxy-5-{[(2-phenylcyclopropyl) carbonyl] amino} benzoic acid) as an initial lead for the development of direct inhibitors of KRAS, a notoriously difficult anticancer drug target. We show that the compound binds to KRAS near the switc...

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Detalles Bibliográficos
Autores principales: Pagba, Cynthia V., Gupta, Amit K., Naji, Ali K., van der Hoeven, Dharini, Churion, Kelly, Liang, Xiaowen, Jakubec, Jacob, Hook, Magnus, Zuo, Yan, Martinez de Kraatz, Marisela, Frost, Jeffrey A., Gorfe, Alemayehu A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10125367/
https://www.ncbi.nlm.nih.gov/pubmed/37101428
http://dx.doi.org/10.1021/acsbiomedchemau.2c00045