Augustyns K, Bal G, Thonus G, Belyaev A, Zhang X M, Bollaert W, Lambeir A M, Durinx C, Goossens F, Haemers A
Department of Pharmaceutical Chemistry, University of Antwerp (UIA), Universiteitsplein 1, Antwerpen, B-2610, Belgium.
Curr Med Chem. 1999 Apr;6(4):311-27.
This review deals with the properties and functions of dipeptidyl peptidase IV (DPP IV, EC 3.4.14.5). This membrane anchored ecto-protease has been identified as the leukocyte antigen CD26. The following aspects of DPP IV/CD26 will be discussed : the structure of DPP IV and the new family of serine proteases to which it belongs, the substrate specificity, the distribution in the human body, specific DPP IV inhibitors and the role of CD26 in the intestinal and renal handling of proline containing peptides, in cell adhesion, in peptide metabolism, in the immune system and in HIV infection. Especially the latest developments in the search for new inhibitors will be reported as well as the discovery of new natural substrates for DPP IV such as the glucagon-like peptides and the chemokines. Finally the therapeutical perspectives for DPP IV inhibitors will be discussed.
本综述探讨了二肽基肽酶IV(DPP IV,EC 3.4.14.5)的性质和功能。这种膜锚定的胞外蛋白酶已被鉴定为白细胞抗原CD26。将讨论DPP IV/CD26的以下方面:DPP IV的结构及其所属的丝氨酸蛋白酶新家族、底物特异性、在人体中的分布、特异性DPP IV抑制剂以及CD26在含脯氨酸肽的肠道和肾脏处理、细胞黏附、肽代谢、免疫系统和HIV感染中的作用。尤其将报道寻找新抑制剂的最新进展以及DPP IV新天然底物(如胰高血糖素样肽和趋化因子)的发现。最后将讨论DPP IV抑制剂的治疗前景。