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Mutant-selective degradation by BRAF-targeting PROTACs

Authors :
Shanique Alabi
Saul Jaime-Figueroa
Zhan Yao
Yijun Gao
John Hines
Kusal T. G. Samarasinghe
Lea Vogt
Neal Rosen
Craig M. Crews
Source :
Nature Communications, Vol 12, Iss 1, Pp 1-11 (2021)
Publication Year :
2021
Publisher :
Nature Portfolio, 2021.

Abstract

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.

Subjects

Subjects :
Science

Details

Language :
English
ISSN :
20411723
Volume :
12
Issue :
1
Database :
Directory of Open Access Journals
Journal :
Nature Communications
Publication Type :
Academic Journal
Accession number :
edsdoj.199e2f0eb92437a873d93ab5b38d197
Document Type :
article
Full Text :
https://doi.org/10.1038/s41467-021-21159-7