Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor

The glucagon-like peptide-1 (GLP-1) receptor is a key regulator of glucose homeostasis and a drug target for type 2 diabetes but available GLP-1R agonists are suboptimal due to several side-effects. Here authors report the cryo-EM structure of GLP-1R bound to an ago-allosteric modulator in complex w...

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Autores principales: Zhaotong Cong, Li-Nan Chen, Honglei Ma, Qingtong Zhou, Xinyu Zou, Chenyu Ye, Antao Dai, Qing Liu, Wei Huang, Xianqiang Sun, Xi Wang, Peiyu Xu, Lihua Zhao, Tian Xia, Wenge Zhong, Dehua Yang, H. Eric Xu, Yan Zhang, Ming-Wei Wang
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Lenguaje:EN
Publicado: Nature Portfolio 2021
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Acceso en línea:https://doaj.org/article/092caffa900241a1b25c21698353ff0d
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spelling oai:doaj.org-article:092caffa900241a1b25c21698353ff0d2021-12-02T17:40:27ZMolecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor10.1038/s41467-021-24058-z2041-1723https://doaj.org/article/092caffa900241a1b25c21698353ff0d2021-06-01T00:00:00Zhttps://doi.org/10.1038/s41467-021-24058-zhttps://doaj.org/toc/2041-1723The glucagon-like peptide-1 (GLP-1) receptor is a key regulator of glucose homeostasis and a drug target for type 2 diabetes but available GLP-1R agonists are suboptimal due to several side-effects. Here authors report the cryo-EM structure of GLP-1R bound to an ago-allosteric modulator in complex with heterotrimeric Gs which offers insights into the molecular details of ago-allosterism.Zhaotong CongLi-Nan ChenHonglei MaQingtong ZhouXinyu ZouChenyu YeAntao DaiQing LiuWei HuangXianqiang SunXi WangPeiyu XuLihua ZhaoTian XiaWenge ZhongDehua YangH. Eric XuYan ZhangMing-Wei WangNature PortfolioarticleScienceQENNature Communications, Vol 12, Iss 1, Pp 1-11 (2021)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
Zhaotong Cong
Li-Nan Chen
Honglei Ma
Qingtong Zhou
Xinyu Zou
Chenyu Ye
Antao Dai
Qing Liu
Wei Huang
Xianqiang Sun
Xi Wang
Peiyu Xu
Lihua Zhao
Tian Xia
Wenge Zhong
Dehua Yang
H. Eric Xu
Yan Zhang
Ming-Wei Wang
Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor
description The glucagon-like peptide-1 (GLP-1) receptor is a key regulator of glucose homeostasis and a drug target for type 2 diabetes but available GLP-1R agonists are suboptimal due to several side-effects. Here authors report the cryo-EM structure of GLP-1R bound to an ago-allosteric modulator in complex with heterotrimeric Gs which offers insights into the molecular details of ago-allosterism.
format article
author Zhaotong Cong
Li-Nan Chen
Honglei Ma
Qingtong Zhou
Xinyu Zou
Chenyu Ye
Antao Dai
Qing Liu
Wei Huang
Xianqiang Sun
Xi Wang
Peiyu Xu
Lihua Zhao
Tian Xia
Wenge Zhong
Dehua Yang
H. Eric Xu
Yan Zhang
Ming-Wei Wang
author_facet Zhaotong Cong
Li-Nan Chen
Honglei Ma
Qingtong Zhou
Xinyu Zou
Chenyu Ye
Antao Dai
Qing Liu
Wei Huang
Xianqiang Sun
Xi Wang
Peiyu Xu
Lihua Zhao
Tian Xia
Wenge Zhong
Dehua Yang
H. Eric Xu
Yan Zhang
Ming-Wei Wang
author_sort Zhaotong Cong
title Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor
title_short Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor
title_full Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor
title_fullStr Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor
title_full_unstemmed Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor
title_sort molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor
publisher Nature Portfolio
publishDate 2021
url https://doaj.org/article/092caffa900241a1b25c21698353ff0d
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