其实司美格鲁肽是针对胰高糖素样肽-1受体 (Glucagon Like Peptide-1Receptor,GLP-1R)靶点研发出的一种GLP-1受体激动剂(GLP-1RA)/ GLP-1类似物,GLP-1是多适应症靶点,接下来,就跟大家聊聊GLP-1你最想知道的那些事儿! 什么是GLP-1? 20世纪60年代,国外学者在研究糖尿病时发现:口服葡萄糖的促胰岛素分泌作用...
[2] Wharton, Sean et al. “Daily Oral GLP-1 Receptor Agonist Orforglipron for Adults with Obesity.” The New England journal of medicine vol. 389,10 (2023): 877-888. doi:10.1056/NEJMoa2302392 [3] Wilding, John P H et al. “Once-Weekly Semaglutide in Adults with Overweight or Obesi...
19 世纪 80 年代 GLP-1 及其生理功能被发现后,科学家便基于 GLP-1 的活性形式GLP-1(7-37)及GLP-1(7-36),amide进行药物开发,而这两种天然的 GLP-1RA 会很快被DPP-4酶解,并在 1-2 min 内被肾脏清除,不具备直接成药性。 GLP-1 成药的问题困扰了科学家数年,直到 1992 年,科学家在 Gila monster 毒...
胰高血糖素样肽-1受体激动剂(glucagon-like peptide-1 receptor agonist, GLP-1 RA)是2型糖尿病治疗领域的一类新型降糖药,随后获得成人超重或肥胖长期体重管理的扩展批准应用。但是,GLP-1 RA在围手术期的安全性仍不确定。有报告称...
1: Y—Z—P, wherein P represents a fragment of a GLP-1 receptor agonist peptide lacking the two N-terminal amino acid residues; and Y—Z represents novel His-Ala mimetics. Examples of GLP-1 receptor agonist compounds are derived from human GLP-1 (7-37), exendin-4(1-39), or GLP-...
1)GLP-1 receptor agonistGLP-1受体激动剂 1.The aim of this project is to establish a GLP-1 signaling pathway targeted cell model, for screening the new class of GLP-1 receptor agonists as anti-diabetic candidates.建立以GLP-1信号通路为靶点的药物筛选细胞模型,用于筛选GLP-1受体激动剂类的新型抗...
之所以会有这种观点,是因为GLP-1R的表达局限性,GLP-1R在免疫细胞中的表达水平较低,然而GLP-1RAs却可以减轻全身性炎症【3】。 近日,来自加拿大多伦多大学的Daniel J. Drucker研究组在Cell Metabolism上发表了研究论文Central glucagon-like peptide 1 r...
英語化学名:GLP-1 receptor agonist 1别名: 1,2,4-Oxadiazol-5(2H)-one, 3-[(1S,2S)-1-[2-[[(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2,3-dihydro-2-oxo-1H-imidazol-1-yl]-2,4,6,7-tetrahydro-4-methyl-5H-pyrazolo[4,3-c]pyridin-5-yl...
United States Patent US8329419 Note: If you have problems viewing the PDF, please make sure you have the latest version ofAdobe Acrobat. Back to full text
Glucagon-like peptide-1 receptor (GLP-1R) activation promotes insulin secretion from pancreatic beta cells, causes weight loss, and is an important pharmacological target in type 2 diabetes (T2D). Like other G protein-coupled receptors, the GLP-1R undergoes agonist-mediated endocytosis, but the fu...