Volume 30, No 12, Dec 2020

ISSN: 1001-0602 
EISSN: 1748-7838 2018 
impact factor 17.848* 
(Clarivate Analytics, 2019)

Volume 30 Issue 12, December 2020: 1140-1142

LETTERS TO THE EDITOR

Structural insights into the activation of GLP-1R by a small molecule agonist

Honglei Ma¹ , Wei Huang² , Xiaoxi Wang¹ , Lihua Zhao¹ , Yi Jiang¹ , Feng Liu³ , Wei Guo² , Xianqiang Sun² , Wenge Zhong² , Daopeng Yuan^2,* , H. Eric Xu^1,*

¹The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
²Qilu Regor Therapeutics Inc., 1206 Zhangjiang Road, Building C, Pu Dong New District, Shanghai 201210, China
³Regor Pharmaceuticals Inc., 50 Soldiers Field Pl, Boston, MA 02135, USA
Correspondence: Daopeng Yuan(Daopeng.yuan@qlregor.com)H. Eric Xu(Eric.xu@simm.ac.cn)

Dear Editor,

The glucagon-like peptide-1 receptor (GLP-1R) belongs to class B G protein-coupled receptors (GPCRs). It is a clinically proven target for type 2 diabetes and obesity.1 Several peptidic drugs have been approved including one in pill form, the oral semaglutide. Despite these advances, oral non-peptidic medicines have been pursued across the pharmaceutical industry for improved patient compliance with reduced side effects such as nausea and vomiting.1 The discovery of non-peptidic drugs has been hampered for many years, primarily owing to the difficulty of mimicking the peptide–receptor interactions with small molecule non-peptidic agonists.

https://doi.org/10.1038/s41422-020-0384-8

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