Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design

G protein-coupled receptors (GPCRs) are a critical target in modern drug development across a wide range of indications. Here the authors provide a comprehensive characterization of a typical GPCR, the angiotensin II (AngII) type 1 receptor (AT1R), and provide insight into its activation mechanism t...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Shaoyong Lu, Xinheng He, Zhao Yang, Zongtao Chai, Shuhua Zhou, Junyan Wang, Ashfaq Ur Rehman, Duan Ni, Jun Pu, Jinpeng Sun, Jian Zhang
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/ac9008e70a2947a995418dd644c36965
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:ac9008e70a2947a995418dd644c36965
record_format	dspace
spelling	oai:doaj.org-article:ac9008e70a2947a995418dd644c369652021-12-02T16:35:46ZActivation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design10.1038/s41467-021-25020-92041-1723https://doaj.org/article/ac9008e70a2947a995418dd644c369652021-08-01T00:00:00Zhttps://doi.org/10.1038/s41467-021-25020-9https://doaj.org/toc/2041-1723G protein-coupled receptors (GPCRs) are a critical target in modern drug development across a wide range of indications. Here the authors provide a comprehensive characterization of a typical GPCR, the angiotensin II (AngII) type 1 receptor (AT1R), and provide insight into its activation mechanism that suggest avenues for the design of allosteric GPCR modulators.Shaoyong LuXinheng HeZhao YangZongtao ChaiShuhua ZhouJunyan WangAshfaq Ur RehmanDuan NiJun PuJinpeng SunJian ZhangNature PortfolioarticleScienceQENNature Communications, Vol 12, Iss 1, Pp 1-15 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Shaoyong Lu Xinheng He Zhao Yang Zongtao Chai Shuhua Zhou Junyan Wang Ashfaq Ur Rehman Duan Ni Jun Pu Jinpeng Sun Jian Zhang Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design
description	G protein-coupled receptors (GPCRs) are a critical target in modern drug development across a wide range of indications. Here the authors provide a comprehensive characterization of a typical GPCR, the angiotensin II (AngII) type 1 receptor (AT1R), and provide insight into its activation mechanism that suggest avenues for the design of allosteric GPCR modulators.
format	article
author	Shaoyong Lu Xinheng He Zhao Yang Zongtao Chai Shuhua Zhou Junyan Wang Ashfaq Ur Rehman Duan Ni Jun Pu Jinpeng Sun Jian Zhang
author_facet	Shaoyong Lu Xinheng He Zhao Yang Zongtao Chai Shuhua Zhou Junyan Wang Ashfaq Ur Rehman Duan Ni Jun Pu Jinpeng Sun Jian Zhang
author_sort	Shaoyong Lu
title	Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design
title_short	Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design
title_full	Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design
title_fullStr	Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design
title_full_unstemmed	Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design
title_sort	activation pathway of a g protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/ac9008e70a2947a995418dd644c36965
work_keys_str_mv	AT shaoyonglu activationpathwayofagproteincoupledreceptoruncoversconformationalintermediatesastargetsforallostericdrugdesign AT xinhenghe activationpathwayofagproteincoupledreceptoruncoversconformationalintermediatesastargetsforallostericdrugdesign AT zhaoyang activationpathwayofagproteincoupledreceptoruncoversconformationalintermediatesastargetsforallostericdrugdesign AT zongtaochai activationpathwayofagproteincoupledreceptoruncoversconformationalintermediatesastargetsforallostericdrugdesign AT shuhuazhou activationpathwayofagproteincoupledreceptoruncoversconformationalintermediatesastargetsforallostericdrugdesign AT junyanwang activationpathwayofagproteincoupledreceptoruncoversconformationalintermediatesastargetsforallostericdrugdesign AT ashfaqurrehman activationpathwayofagproteincoupledreceptoruncoversconformationalintermediatesastargetsforallostericdrugdesign AT duanni activationpathwayofagproteincoupledreceptoruncoversconformationalintermediatesastargetsforallostericdrugdesign AT junpu activationpathwayofagproteincoupledreceptoruncoversconformationalintermediatesastargetsforallostericdrugdesign AT jinpengsun activationpathwayofagproteincoupledreceptoruncoversconformationalintermediatesastargetsforallostericdrugdesign AT jianzhang activationpathwayofagproteincoupledreceptoruncoversconformationalintermediatesastargetsforallostericdrugdesign
_version_	1718383711931596800

Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design

Ejemplares similares