顾名思义,GLP-1R的主要作用是和胰高血糖素样肽-1(glucagon-like peptide-1 receptor, GLP-1)结合,调节血糖。 图2 GLP-1R跨膜区三维结构 GLP-1 GLP-1是一种主要由肠道L细胞所产生的激素,属于肠促胰素。GLP-1的半衰期非常短,仅1-2min,其发挥生理功能主要是通过结合并激活GLP-1R。人体内肠促胰素除GLP-1...
[11] Wan, W.; Qin, Q.; Xie, L.; et al. GLP-1R Signaling and Functional Molecules in Incretin Therapy. Molecules 2023, 28, 751.[12] Bavec, A.; Hallbrink, M.; Langel, U.; et al. Different role of intracellular loops of glucagon-like peptide-1 receptor in G-protein coupling....
D.J., Husain, M. 2008. Cardioprotective and vasodilatory actions of glucagon-like peptide 1 receptor are mediated through both glucagon-like peptide 1 receptor-dependent and independent pathways. Circulation 117:2340-2350.
D.J., Husain, M. 2008. Cardioprotective and vasodilatory actions of glucagon-like peptide 1 receptor are mediated through both glucagon-like peptide 1 receptor-dependent and independent pathways. Circulation 117:2340-2350.
[2] Wei, Y., Mojsov, S. 1995. Tissue-specific expression of the human receptor for glucagon-like peptide-I: brain, heart and pancreatic forms have the same deduced amino acid sequences. FEBS Lett 358:219-224. [...
[18] Li, Y., Hansotia, T., Yusta, B., Ris, F., Halban, P.A., Drucker, D.J. 2003. Glucagon-like peptide-1 receptor signaling modulates beta cell apoptosis. J Biol Chem 278:471-478. [19] Park, S., Dong, X., Fisher, T.L., Dunn, S., Omer, A.K., Weir, G., et al...
自胰高糖素样肽-1(GLP-1)被发现以来,它已然成为一种“多面手”激素——其多种代谢功能被人们发现,远远超出了作为肠促胰素的经典定义。GLP-1的众多有益的靶点作用使其受体激动剂逐渐成为更多新兴的治疗领域如脂肪肝、肥胖和神经退行性疾病等的冉冉之“星”药物。时值利拉鲁肽在我国上市10周年,司美格鲁肽新上市之...
人的GLP-1R基因位于第6号染色体上,编码463个氨基酸。胰腺内的GLP-1R主要表达在胰岛β细胞中,除胰岛外,GLP-1R还广泛表达于胃、小肠、心脏、肾脏、肺及大脑等组织器官中[3]。顾名思义,GLP-1R的主要作用是和胰高血糖素样肽-1(glucagon-like peptide-1 receptor, GLP-1)结合,调节血糖。
[8] Wei, R. et al. Exenatide exerts direct protective effects on endothelial cells through the AMPK/Akt/eNOS pathway in a GLP-1 receptor-dependent manner. Am J Physiol Endocrinol Metab. 2016, 310, E947-E957. [9] Lee, ...
[18] Li, Y., Hansotia, T., Yusta, B., Ris, F., Halban, P.A., Drucker, D.J. 2003. Glucagon-like peptide-1 receptor signaling modulates beta cell apoptosis. J Biol Chem 278:471-478. [19] Park, S., Dong, X., Fi...