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.
Enregistré dans:
Auteurs principaux: | Shanique Alabi, Saul Jaime-Figueroa, Zhan Yao, Yijun Gao, John Hines, Kusal T. G. Samarasinghe, Lea Vogt, Neal Rosen, Craig M. Crews |
---|---|
Format: | article |
Langue: | EN |
Publié: |
Nature Portfolio
2021
|
Sujets: | |
Accès en ligne: | https://doaj.org/article/c199e2f0eb92437a873d93ab5b38d197 |
Tags: |
Ajouter un tag
Pas de tags, Soyez le premier à ajouter un tag!
|
Documents similaires
-
Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
par: Blake E. Smith, et autres
Publié: (2019) -
IGF1R/IR Mediates Resistance to BRAF and MEK Inhibitors in BRAF-Mutant Melanoma
par: Hima Patel, et autres
Publié: (2021) -
Potential application of proteolysis targeting chimera (PROTAC) modification technology in natural products for their targeted protein degradation
par: Guliang Yang, et autres
Publié: (2022) -
Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation
par: Chiara Maniaci, et autres
Publié: (2017) -
Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry
par: Wen-Hao Guo, et autres
Publié: (2020)