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。
[2]Is retatrutide (LY3437943), a GLP-1, GIP, and glucagon receptor agonist a step forward in thetreatment of diabetes and obesity? [3]LY3437943, a novel triple GIP, GLP-1, and glucagon receptor agonist in p...
[2]Is retatrutide (LY3437943), a GLP-1, GIP, and glucagon receptor agonist a step forward in the treatment of diabetes and obesity? [3]LY3437943, a novel triple GIP, GLP-1, and glucagon receptor agonist in people with type 2 diabetes: a phase 1b, multicentre, double-blind, placebo-...
Pocai A. Action and therapeutic potential of oxyntomodulin. Mol Metab. 2013 Dec 14;3(3):241-51. Zhihong Y,etc. Emerging roles of oxyntomodulin-based glucagon-like peptide-1/glucagon co-agonist analogs in diabetes and obesity. Peptides. 2023 Apr;162:170955. 雷春涛等. 胃泌酸调节素对体重及...
Zhihong Y,etc. Emerging roles of oxyntomodulin-based glucagon-like peptide-1/glucagon co-agonist analogs in diabetes and obesity. Peptides. 2023 Apr;162:170955. 雷春涛等. 胃泌酸调节素对体重及糖代谢影响的研究进展[J]...
3.ROBERT AUGUSTIN, et al. Selection of BI 456906 as a Dual GCGR/GLP-1R Agonist Based on In Vitro Potency and In Vivo Target Engagement Biomarkers. Diabetes 2023;72(Supplement_1):749-P.
Zhihong Y,etc. Emerging roles of oxyntomodulin-based glucagon-like peptide-1/glucagon co-agonist analogs in diabetes and obesity. Peptides. 2023 Apr;162:170955. 雷春涛等. 胃泌酸调节素对体重及糖代谢影响的研究进展[J]. 中华临床医师杂志(电子版),2013(24):11771-11774. ...
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 ...
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...
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. 2024;12(3):162-173. ...