Dissecting RAF inhibitor resistance by structure-based modeling reveals ways to overcome oncogenic RAS signaling

Clinically used RAF inhibitors are ineffective in RAS-mutant tumors because they enhance homo- and heterodimerization of RAF kinases, leading to paradoxical activation of ERK signaling. Overcoming enhanced RAF dimerization and the resulting resistance is a challenge for drug design. Combining multip...

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Pubblicato in:Cell Syst
Autori principali: Rukhlenko, Oleksii S., Khorsand, Fahimeh, Krstic, Aleksandar, Rozanc, Jan, Alexopoulos, Leonidas G., Rauch, Nora, Erickson, Keesha E., Hlavacek, William S., Posner, Richard G., Gómez-Coca, Silvia, Rosta, Edina, Fitzgibbon, Cheree, Matallanas, David, Rauch, Jens, Kolch, Walter, Kholodenko, Boris N.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2018
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC6149545/
https://ncbi.nlm.nih.gov/pubmed/30007540
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.cels.2018.06.002
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