RAF inhibitors promote RAS-RAF interaction by allosterically disrupting RAF autoinhibition

First-generation RAF inhibitors paradoxically induce ERK signaling in normal and tumor cells exhibiting RAS activity. Compound-induced RAF dimerization through stabilization of the RAF ON/active state by inhibitors has emerged as a critical contributing factor. RAF inhibitors also enhance RAS−RAF as...

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Detalles Bibliográficos
Autores principales: Jin, Ting, Lavoie, Hugo, Sahmi, Malha, David, Maud, Hilt, Christine, Hammell, Amy, Therrien, Marc
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2017
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5662619/
https://www.ncbi.nlm.nih.gov/pubmed/29084939
http://dx.doi.org/10.1038/s41467-017-01274-0

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5662619/
https://www.ncbi.nlm.nih.gov/pubmed/29084939
http://dx.doi.org/10.1038/s41467-017-01274-0

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