化学
变构调节
小分子
肠促胰岛素
胰高血糖素样肽-1
药理学
计算生物学
糖尿病
受体
生物化学
医学
2型糖尿病
内分泌学
生物
作者
Haibo Zhang,Tianxiao Wu,Yong Wu,Yuran Peng,Xian Hong Wei,Tao Lü,Yu Jiao
标识
DOI:10.1016/j.ejmech.2024.116632
摘要
Glucagon-like peptide-1 receptor (GLP-1R) is a pivotal receptor involved in blood glucose regulation and influencing feeding behavior. It has received significant attention in the treatment of obesity and diabetes due to its potent incretin effect. Peptide GLP-1 receptor agonists (GLP-1RAs) have achieved tremendous success in the market, driving the vigorous development of small molecule GLP-1RAs. Currently, several small molecules have entered the clinical research stage. Additionally, recent discoveries of GLP-1R positive allosteric modulators (PAMs) are also unveiling new regulatory patterns and treatment methods. This article reviews the structure and functional mechanisms of GLP-1R, recent reports on small molecule GLP-1RAs and PAMs, as well as the optimization process. Furthermore, it combines computer simulations to analyze structure-activity relationships (SAR) studies, providing a foundation for exploring new strategies for designing small molecule GLP-1RAs.
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