Mutant-selective degradation by BRAF-targeting PROTACs

Hundreds of BRAF mutations have been identified in patients with cancer but currently approved drugs only target BRAF V600 mutants. Here, the authors develop a vemurafenib-based PROTAC that induces degradation of all classes of BRAF mutants without affecting wild-type RAF proteins.

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Bibliographic Details
Main Authors: Shanique Alabi, Saul Jaime-Figueroa, Zhan Yao, Yijun Gao, John Hines, Kusal T. G. Samarasinghe, Lea Vogt, Neal Rosen, Craig M. Crews
Format: article
Language:EN
Published: Nature Portfolio 2021
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Online Access:https://doaj.org/article/c199e2f0eb92437a873d93ab5b38d197
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Summary:Hundreds of BRAF mutations have been identified in patients with cancer but currently approved drugs only target BRAF V600 mutants. Here, the authors develop a vemurafenib-based PROTAC that induces degradation of all classes of BRAF mutants without affecting wild-type RAF proteins.