在胰腺中,目前认为GLP-1R主要通过Gαs /cAMP 通路发出信号,但有证据表明GLP-1R也与Gαq和其他G蛋白偶联。GLP-1R激活后,C末端发生磷酸化,进一步募集β-arrestin,导致受体内化和脱敏。Gαs/cAMP通路可直接引发葡萄糖诱导的胰岛素颗粒分泌。GLP-1R完全激活后,会与Gαs进行偶联并激活腺苷酸环化酶(AC),使A...
品名:PathHunter CHO-K1 mGLP1R Beta-Arrestin-1 Cell Line 规格:Clone 货号:93-0974C2 一、我们关于PathHunter CHO-K1 mGLP1R Beta-Arrestin-1 Cell Line蛋白、试剂盒、补体的声明 我们致力于成为科研试剂搜索、采购一体化解决方案提供商! 我们是一家致力于为生命科学研究、研发及生物技术公司提供上等、蛋白及检...
Beta-Arrestin-1 mediates glucagon-like peptide-1 signaling to insulin secretion in cultured pancreatic beta cells[J]. Proceedings of the National Academy of Sciences of the United States of America, 2008, 105 :6614- 6619. [40]Shukla AK, Xiao K, Lefkowitz RJ. Emerging paradigms of β-...
目前认为GLP1R主要通过Gαs/cAMP通路发出信号;然而,有证据表明GLP1R与Gαq和其他G蛋白偶联。激活后,GLP1R在C端发生磷酸化,进一步募集β-arrestin,导致受体内化和脱敏。Gαs/cAMP途径直接导致葡萄糖诱导的胰岛素颗粒分泌。在被GLP-1等完
[94] Sonoda, N., Imamura, T., Yoshizaki, T., Babendure, J.L., Lu, J.C., Olefsky, J.M. 2008. Beta-Arrestin-1 mediates glucagon-like peptide-1 signaling to insulin secretion in cultured pancreatic beta cells. Proc Natl Acad Sci U S A 105:6614-6619. ...
[94] Sonoda, N., Imamura, T., Yoshizaki, T., Babendure, J.L., Lu, J.C., Olefsky, J.M. 2008. Beta-Arrestin-1 mediates glucagon-like peptide-1 signaling to insulin secretion in cultured pancreatic beta...
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[95] Quoyer, J., Longuet, C., Broca, C., Linck, N., Costes, S., Varin, E., et al. 2010. GLP-1 mediates antiapoptotic effect by phosphorylating Bad through a beta-arrestin 1-mediated ERK1/2 activation in pancreatic beta-cells. J Biol Chem 285:1989-2002. ...
et al. Lack of beta-arrestin signaling in the absence of active G proteins. Nat. Commun. 9, 341 (2018). Article ADS PubMed PubMed Central Google Scholar Furness, S. G. B. et al. Ligand-dependent modulation of G protein conformation alters drug efficacy. Cell 167, 739–749 e711 (...
GLP-1R beta arrestin-2 recruitment was lower with HISHS-2001, indicating increased bias. Efficacy and potency of recruitment of Gs protein to the GLP-1R were lower for HISHS-2001 vs. tirzepatide (Table). HISHS-2001 showed increased potency for Gs recruitment to the GIPR. GLP...