组织蛋白酶及其抑制剂研究进展

Cathepsins:Structures,Functions and Inhibitors

组织蛋白酶是半胱氨酸蛋白酶家族的主要成员,在生物界已发现20余种,人体中主要存在11种,它们与人类肿瘤、骨质疏松、关节炎等多种重大疾病密切相关,是近年来备受关注的一类靶标蛋白酶。自从20世纪90年代以来,多种组织蛋白酶的晶体结构陆续明确,有关其研究进展较快。本文以人类组织蛋白酶为重点,主要介绍近15年来组织蛋白酶结构、功能和抑制剂研究方面的一些重要进展。

Cathepsins are the main members of the cysteine pmtease family. Up to now, more than 20 cathepsins have been discovered in living organisms including 11 human cathepsins, which are involved in many serious human diseases, such as tumor, osteopomsis, arthritis and so on. So cathepsins may represent important drug targets with more attention. Since 1990, the crystal structures of several cathepsins were obtained respectively, the research about them progressed much. This paper summarized recent developments in structures, functions and inhihitors of cathepsins, especially human cathepsins.