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二肽基肽酶-Ⅳ(Dipeptidyl Peptidase-IV,DPP-Ⅳ)是一个以同型二聚体形式存在于细胞膜上的多功能酶。它可以裂解包括胰高血糖素样肽-1(glucagons-like peptide 1,GLP-1)和抑胃肽(glucose-denpen-dent insulinotropic polypeptide,GIP)在内的多种肽类激素,而后两者与2型糖尿病有着密切联系。作为治疗糖尿病药物的一个新靶标,DPP-Ⅳ近年来受到极大关注。伴随着第一个DPP-Ⅳ抑制剂西他列汀(sitagliptin)在美国的上市,科研工作者对DPP-Ⅳ的研究也越来越深入。文中从DPP-Ⅳ分子的结构、分布、功能等方面进行了介绍,并对目前DPP-Ⅳ抑制剂的研发现状、临床作用及其机制的研究进展进行了综述。
Dipeptidyl Peptidase-IV (DPP-IV) is a multifunctional enzyme that exists as a homodimer on the cell membrane. It cleaves multiple peptide hormones, including glucagons-like peptide 1 (GLP-1) and glucose-denpen-dent insulinotropic polypeptide (GIP) With type 2 diabetes are closely linked. As a new target for the treatment of diabetes drugs, DPP-IV has drawn great attention in recent years. With the listing of sitagliptin, the first DPP-IV inhibitor, in the United States, research on DPP-IV by researchers has also deepened. In this paper, we introduced the structure, distribution and function of DPP-Ⅳ, and summarized the current research status, clinical function and mechanism of DPP-Ⅳ inhibitors.