Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

PROTACs enable targeted protein degradation by recruiting an E3 ligase to a specific substrate but the determinants of selectivity are not fully understood. Here, the authors show that varying the linker between warhead and E3 ligand and the orientation of the E3 ligase allow tuning PROTAC selectivi...

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Autores principales:	Blake E. Smith, Stephen L. Wang, Saul Jaime-Figueroa, Alicia Harbin, Jing Wang, Brian D. Hamman, Craig M. Crews
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2019
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/86ec9e4d91cb498bb96bd2e90667c3f4
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spelling	oai:doaj.org-article:86ec9e4d91cb498bb96bd2e90667c3f42021-12-02T17:31:37ZDifferential PROTAC substrate specificity dictated by orientation of recruited E3 ligase10.1038/s41467-018-08027-72041-1723https://doaj.org/article/86ec9e4d91cb498bb96bd2e90667c3f42019-01-01T00:00:00Zhttps://doi.org/10.1038/s41467-018-08027-7https://doaj.org/toc/2041-1723PROTACs enable targeted protein degradation by recruiting an E3 ligase to a specific substrate but the determinants of selectivity are not fully understood. Here, the authors show that varying the linker between warhead and E3 ligand and the orientation of the E3 ligase allow tuning PROTAC selectivity toward different p38 isoforms.Blake E. SmithStephen L. WangSaul Jaime-FigueroaAlicia HarbinJing WangBrian D. HammanCraig M. CrewsNature PortfolioarticleScienceQENNature Communications, Vol 10, Iss 1, Pp 1-13 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Blake E. Smith Stephen L. Wang Saul Jaime-Figueroa Alicia Harbin Jing Wang Brian D. Hamman Craig M. Crews Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
description	PROTACs enable targeted protein degradation by recruiting an E3 ligase to a specific substrate but the determinants of selectivity are not fully understood. Here, the authors show that varying the linker between warhead and E3 ligand and the orientation of the E3 ligase allow tuning PROTAC selectivity toward different p38 isoforms.
format	article
author	Blake E. Smith Stephen L. Wang Saul Jaime-Figueroa Alicia Harbin Jing Wang Brian D. Hamman Craig M. Crews
author_facet	Blake E. Smith Stephen L. Wang Saul Jaime-Figueroa Alicia Harbin Jing Wang Brian D. Hamman Craig M. Crews
author_sort	Blake E. Smith
title	Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
title_short	Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
title_full	Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
title_fullStr	Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
title_full_unstemmed	Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
title_sort	differential protac substrate specificity dictated by orientation of recruited e3 ligase
publisher	Nature Portfolio
publishDate	2019
url	https://doaj.org/article/86ec9e4d91cb498bb96bd2e90667c3f4
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_version_	1718380565519925248

Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

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