Progress in research on small molecule glucagon-like peptide-1 receptor agonists
ZHANG Xin-yi
WANG Tian-min
CHEN Yin-bo
ZHANG Peng
ZHU Xue-yan
Abstract：The glucagon-like peptide-1 receptor(GLP-1R)is an important therapeutic target for type 2 diabetes mellitus(T2DM).Drugs targeting GLP-1R,an emerging target,exhibit several unique advantages compared to drugs against traditional targets.The success of representative drugs such as semaglutide has drawn significant attention from numerous companies and individual research institutions.However,the currently marketed drugs in this field are predominantly peptide-based.Small molecule drugs,which can address some of the inherent limitations of peptide-based drugs,have become a popular direction in diabetes research.This article summarizes the known small-molecule GLP-1R agonists and systematically elaborates on their research background,characteristics,and activity,aiming to provide insights for further exploration of treatment strategies for T2DM.
Keywords：glucagon-like peptide-1 receptorsmall molecule glucagon-like peptide-1 receptor agonistallosteric glucagon-like peptide-1 receptor modulatorbiased agonist
Publication Date：2025-06-30
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：7( 1269-1275 )