Mazdutide is the first GLP-1R/GCGR dual agonist in the regulatory review status, with a first new drug application (NDA) for chronic weight management and a second NDA for T2D currently under review by the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA...
4.le Roux CW, Steen O, Lucas KJ, et al. Glucagon and GLP-1 receptor dual agonist survodutide for obesity: a randomised, double-blind, placebo-controlled, dose-finding phase 2 trial. Lancet Diabetes Endocrinol. 2...
and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept》中,提出了LY3437943 (LY)(图1A)化合物,是一种由GIP肽主链改造而成脂肪酸酰化的单肽,在GCGR、GIPR和GLP-1R上具有三重激动剂的活性,通过调节GCGR、GIPR和GLP-1R的活性对代谢产生益处。
The invention relates to uses of polypeptide compounds having dual target agonist effect on glucagon-like peptide-1 receptor (GLP-1R) and glucagon receptor (GCGR). Characterized by high enzymolysis stability, high biological activity and no adverse reaction, the polypeptide compounds are capable of ...
1. Selvarajah V, Robertson D, Hansen L, et al. A randomized phase 2b trial examined the effects of the glucagon-like peptide-1 and glucagon receptor agonist cotadutide on kidney outcomes in patients with diabetic kidney dis...
与传统的“Agonist-first”模式相比，这种“G protein-first”模式或能使受体在结合配体后被更快地激活。综上，该研究通过GLP-1R、GCGR和GIPR的“裸奔”结构揭示了B1类GPCR激活中的过渡态，即激活前G蛋白之预偶联，为深入认识GPCR激活机制和信号转导提供了新的信息。复旦大学基础医学院研究助理丛朝彤和中国科学院...
1. Sanyal AJ, Bedossa P, Fraessdorf M, et al. Glucagon and GLP-1 receptor dual agonist Survodutide improved liver histology in people with MASH and fibrosis: Results from a randomized, double-blind, placebo-controlled phase 2 trial. EASL 2024 oral. ...
Design of a highly potent GLP-1R and GCGR dual-agonist for recovering hepatic fibrosis Nazi Song, Hongjiao Xu, Jiahua Liu, Qian Zhao, Hui Chen,ZhibinYan,Runling Yang,ZhitengLuo,QiLiu,JianmeiOuyang,ShuohanWu,SuijiaLuo,ShuyinYe,RunfengLin,Xi Sun,JunqiuXie,TianLan,Zhongdao Wu*,Rui Wang*,Xian...
This reporter cell was incubated with serial dilutions of Tirzepatide (a dual GLP-1R and GIPR agonist). The EC50 of Tirzepatide was approximately 0.042 nM. This reporter cell was incubated with serial dilutions of Tirzepatide (a dual GLP-1R and GIPR agonist). The max induction fold was...
参考文献:Mazen Noureddin, Corinna Schoelch, Elisabetta Bugianesi, et al. Analysis of noninvasive liver biomarkers in a phase II trial of the glucagon and glp-1 receptor dual agonist survodutide in people with metabolic dysfunction associated steatohepatitis (MASH) and fibrosis. AASLD 2024 Abstrac...