摘要
Exendin-4是一种胰高血糖素样肽-1(GLP-1)受体的长效激动剂,与GLP-1具有53%的序列同源性,具有促进葡萄糖依赖性的胰岛素分泌、促进β细胞增殖、减慢胃排空、抑制食物摄取和减轻体重等作用,有望成为治疗2型糖尿病的理想药物。综述Exendin-4的结构、药理作用、制备方法、结构修饰改造的策略,介绍首个用于临床的Exendin-4类药物Exenatide,并对Exendin-4及其类似物的发展前景进行了展望。
Exendin-4 is a long-acting agonist of mammalian glucagon-like peptide-1 （GLP-1） receptor, which has a 53 % amino acid sequence overlap with GLP-1. Its activities include glucose-dependent stimulation of insulin secretion, enhancement of β-cell mass, slowing of gastric emptying, inhibition of food intake and body weight loss, and it is hopeful to be appraised as a potential drug for type 2 diabetes. This article reviews the structure, pharmacological activity, production and structural alteration of Exendin-4, and introduces the future development of Exendin-4 and its analogs, including the first clinical drug ＂Exenatide＂.
出处
《药学进展》
CAS
2007年第9期403-407,共5页
Progress in Pharmaceutical Sciences
