Nature Communications (Jun 2021)
Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor
- 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
Affiliations
- Zhaotong Cong
- School of Pharmacy, Fudan University
- Li-Nan Chen
- Department of Biophysics and Department of Pathology of Sir Run Run Shaw Hospital, Zhejiang University School of Medicine
- Honglei Ma
- The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- Qingtong Zhou
- School of Basic Medical Sciences, Fudan University
- Xinyu Zou
- School of Artificial Intelligence and Automation, Huazhong University of Science and Technology
- Chenyu Ye
- School of Pharmacy, Fudan University
- Antao Dai
- The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- Qing Liu
- The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- Wei Huang
- Qilu Regor Therapeutics, Inc.
- Xianqiang Sun
- Qilu Regor Therapeutics, Inc.
- Xi Wang
- The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- Peiyu Xu
- The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- Lihua Zhao
- The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- Tian Xia
- School of Artificial Intelligence and Automation, Huazhong University of Science and Technology
- Wenge Zhong
- Qilu Regor Therapeutics, Inc.
- Dehua Yang
- The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- H. Eric Xu
- The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- Yan Zhang
- Department of Biophysics and Department of Pathology of Sir Run Run Shaw Hospital, Zhejiang University School of Medicine
- Ming-Wei Wang
- School of Pharmacy, Fudan University
- DOI
- https://doi.org/10.1038/s41467-021-24058-z
- Journal volume & issue
-
Vol. 12,
no. 1
pp. 1 – 11
Abstract
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.
