生物活性

• 描述Glucagon-like peptide-1 (GLP-1) is an enteroendocrine hormone that has a capacity, when administered exogenously, to normalize blood glucose levels in type 2 diabetes mellitus. Exendin-4, a 39-amino acid (AA) peptide, is a long-acting agonist at the GLP-1 receptor with an IC₅₀ value of 3.22 nM^[3]. In human umbilical vein endothelial cells (HUVECs), exendin-4 significantly increased NO production, endothelial NO synthase (eNOS) phosphorylation, and GTP cyclohydrolase 1 (GTPCH1) level in a dose-dependent manner^[4]. In vivo, ob/ob mice sustained a reduction in the net weight gained during exendin-4 treatment (10 μg/kg or 20 μg/kg for 60 days). Furthermore, serum glucose and hepatic steatosis was significantly reduced and insulin sensitivity was improved in exendin-4 treated ob/ob mice^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02541734	Diabetes Mellitus, Non-Insulin... more >>-Dependent Diabetes Mellitus Collapse <<	Phase 1 Phase 2	Completed	-	-
  NCT03444142	Diabetes Mellitus, Type 2	Phase 4	Recruiting	December 30, 2018	Mexico ... more >> Instituto de terapeutica Experimental y Clinica. Centro universitario de Ciencias de la Salud. Universidad de Guadalajara Recruiting Guadalajara, Jalisco, Mexico, 44340 Collapse <<
  NCT00516048	Type 2 Diabetes Mellitus	Phase 3	Completed	-	Australia, South Australia ... more >> Research Site Keswick, South Australia, Australia Canada, Alberta Research Site Calgary, Alberta, Canada Canada, British Columbia Research Site Vancouver, British Columbia, Canada Canada, Ontario Research Site London, Ontario, Canada Hungary Research Site Budapest, Hungary Research Site Gyula, Hungary Research Site Zalaegerszeg, Hungary Italy Research Site Milan, Italy Research Site Perugia, Italy Research Site Rome, Italy Korea, Republic of Research Site Seonnam City, Korea, Republic of Research Site Seoul, Korea, Republic of Research Site Suwon City, Korea, Republic of Collapse <<

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• 参考文献

• [1] Tsutsumi Y, Nomiyama T, et al. Combined Treatment with Exendin-4 and Metformin Attenuates Prostate Cancer Growth. PLoS One. 2015 Oct 6;10(10):e0139709.

  [2] Zhou Y, He X, et al. Exendin-4 attenuates cardiac hypertrophy via AMPK/mTOR signaling pathway activation. Biochem Biophys Res Commun. 2015 Dec 4-11;468(1-2):394-9.

  [3] Doyle ME, Theodorakis MJ, et al. The importance of the nine-amino acid C-terminal sequence of exendin-4 for binding to the GLP-1 receptor and for biological activity. Regul Pept. 2003 Jul 15;114(2-3):153-8

  [4] Wei R, Ma S, Wang C, 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 Jun 1;310(11):E947-57

  [5] Ding X, Saxena NK, Lin S, Gupta NA, Anania FA. Exendin-4, a glucagon-like protein-1 (GLP-1) receptor agonist, reverses hepatic steatosis in ob/ob mice. Hepatology. 2006 Jan;43(1):173-81

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