Path Forward for RAF Therapies: Inhibition of Monomers and Dimers

Current BRAF inhibitors block signaling from monomeric BRAFV600E, but not from oncogenic RAS, which requires RAF dimerization. In this issue of Cancer Cell, Yao and colleagues investigate why current drugs are ineffective against RAF dimers, while Peng and colleagues describe a pan-RAF inhibitor tar...

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Bibliographic Details
Published in:Cancer cell 2015-09, Vol.28 (3), p.279-281
Main Authors: Kortum, Robert L., Morrison, Deborah K.
Format: Article
Language:English
Subjects:
Humans
MAP Kinase Signaling System - drug effects
MAP Kinase Signaling System - genetics
Mutation - genetics
Protein Kinase Inhibitors - pharmacology
Proto-Oncogene Proteins B-raf - antagonists & inhibitors
Proto-Oncogene Proteins B-raf - genetics
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Summary:Current BRAF inhibitors block signaling from monomeric BRAFV600E, but not from oncogenic RAS, which requires RAF dimerization. In this issue of Cancer Cell, Yao and colleagues investigate why current drugs are ineffective against RAF dimers, while Peng and colleagues describe a pan-RAF inhibitor targeting both monomeric and dimeric RAF. Current BRAF inhibitors block signaling from monomeric BRAFV600E, but not from oncogenic RAS, which requires RAF dimerization. In this issue of Cancer Cell, Yao and colleagues elucidate why current drugs are ineffective against RAF dimers, while Peng and colleagues describe a pan-RAF inhibitor targeting both monomeric and dimeric RAF.
ISSN:1535-6108
1878-3686
DOI:10.1016/j.ccell.2015.08.006