Inhibitors of BRAF dimers using an allosteric site
oleh: Xiomaris M. Cotto-Rios, Bogos Agianian, Nadege Gitego, Emmanouil Zacharioudakis, Orsi Giricz, Yang Wu, Yiyu Zou, Amit Verma, Poulikos I. Poulikakos, Evripidis Gavathiotis
| Format: | Article |
|---|---|
| Diterbitkan: | Nature Portfolio 2020-09-01 |
Deskripsi
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.