Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization

RAF kinases play a prominent role in cancer. Their mode of activation is complex, but critically requires dimerization of their kinase domains. Unexpectedly, several ATP-competitive RAF inhibitors were recently found to promote dimerization and transactivation of RAF kinases in a RAS-dependent manne...

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Udgivet i:Nat Chem Biol
Main Authors: Lavoie, Hugo, Thevakumaran, Neroshan, Gavory, Gwenaëlle, Li, John, Padeganeh, Abbas, Guiral, Sébastien, Duchaine, Jean, Mao, Daniel Y. L., Bouvier, Michel, Sicheri, Frank, Therrien, Marc
Format: Artigo
Sprog:Inglês
Udgivet: 2013
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Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4954776/
https://ncbi.nlm.nih.gov/pubmed/23685672
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/nchembio.1257
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