Inhibitors of BRAF dimers using an allosteric site

Autor: Xiomaris M. Cotto-Rios, Bogos Agianian, Nadege Gitego, Emmanouil Zacharioudakis, Orsi Giricz, Yang Wu, Yiyu Zou, Amit Verma, Poulikos I. Poulikakos, Evripidis Gavathiotis
Jazyk: angličtina
Rok vydání: 2020
Předmět:
Zdroj: Nature Communications, Vol 11, Iss 1, Pp 1-16 (2020)
Druh dokumentu: article
ISSN: 2041-1723
DOI: 10.1038/s41467-020-18123-2
Popis: FDA-approved RAF inhibitors poorly inhibit BRAF dimers, which limits their clinical efficacy in tumors expressing BRAFV600E mutant monomers. Here the authors identify FDA-approved Ponatinib as an effective inhibitor of BRAF monomers and dimers and designed PHI1, an inhibitor with a unique mode of action and selectivity for oncogenic BRAF dimers.
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