Mechanism of dimer selectivity and binding cooperativity of BRAF inhibitors

Aberrant signaling of BRAFV600E is a major cancer driver. Current FDA-approved RAF inhibitors selectively inhibit the monomeric BRAFV600E and suffer from tumor resistance. Recently, dimer-selective and equipotent RAF inhibitors have been developed; however, the mechanism of dimer selectivity is poor...

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Main Authors: Joseph Clayton, Aarion Romany, Evangelia Matenoglou, Evripidis Gavathiotis, Poulikos I Poulikakos, Jana Shen
Format: Article
Language:English
Published: eLife Sciences Publications Ltd 2025-02-01
Series:eLife
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Online Access:https://elifesciences.org/articles/95334
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