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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Autores principales:	Shanique Alabi, Saul Jaime-Figueroa, Zhan Yao, Yijun Gao, John Hines, Kusal T. G. Samarasinghe, Lea Vogt, Neal Rosen, Craig M. Crews
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/c199e2f0eb92437a873d93ab5b38d197
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spelling	oai:doaj.org-article:c199e2f0eb92437a873d93ab5b38d1972021-12-02T14:11:09ZMutant-selective degradation by BRAF-targeting PROTACs10.1038/s41467-021-21159-72041-1723https://doaj.org/article/c199e2f0eb92437a873d93ab5b38d1972021-02-01T00:00:00Zhttps://doi.org/10.1038/s41467-021-21159-7https://doaj.org/toc/2041-1723Hundreds 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.Shanique AlabiSaul Jaime-FigueroaZhan YaoYijun GaoJohn HinesKusal T. G. SamarasingheLea VogtNeal RosenCraig M. CrewsNature PortfolioarticleScienceQENNature Communications, Vol 12, Iss 1, Pp 1-11 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Shanique Alabi Saul Jaime-Figueroa Zhan Yao Yijun Gao John Hines Kusal T. G. Samarasinghe Lea Vogt Neal Rosen Craig M. Crews Mutant-selective degradation by BRAF-targeting PROTACs
description	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.
format	article
author	Shanique Alabi Saul Jaime-Figueroa Zhan Yao Yijun Gao John Hines Kusal T. G. Samarasinghe Lea Vogt Neal Rosen Craig M. Crews
author_facet	Shanique Alabi Saul Jaime-Figueroa Zhan Yao Yijun Gao John Hines Kusal T. G. Samarasinghe Lea Vogt Neal Rosen Craig M. Crews
author_sort	Shanique Alabi
title	Mutant-selective degradation by BRAF-targeting PROTACs
title_short	Mutant-selective degradation by BRAF-targeting PROTACs
title_full	Mutant-selective degradation by BRAF-targeting PROTACs
title_fullStr	Mutant-selective degradation by BRAF-targeting PROTACs
title_full_unstemmed	Mutant-selective degradation by BRAF-targeting PROTACs
title_sort	mutant-selective degradation by braf-targeting protacs
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/c199e2f0eb92437a873d93ab5b38d197
work_keys_str_mv	AT shaniquealabi mutantselectivedegradationbybraftargetingprotacs AT sauljaimefigueroa mutantselectivedegradationbybraftargetingprotacs AT zhanyao mutantselectivedegradationbybraftargetingprotacs AT yijungao mutantselectivedegradationbybraftargetingprotacs AT johnhines mutantselectivedegradationbybraftargetingprotacs AT kusaltgsamarasinghe mutantselectivedegradationbybraftargetingprotacs AT leavogt mutantselectivedegradationbybraftargetingprotacs AT nealrosen mutantselectivedegradationbybraftargetingprotacs AT craigmcrews mutantselectivedegradationbybraftargetingprotacs
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Mutant-selective degradation by BRAF-targeting PROTACs

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