Abstract: Human carbonic anhydrase Ⅱ is one of the most efficient one in carbonic anhydrase isozymes, which catalyzes the reversible hydration dehydration of CO2 and water : CO₂ + H₂O\ HCO₃^- + H⁺. It is found in virtually every tissue
and cell type, and involves in many human physiological and pathological processes, such as human acid-base balance, glaucoma, osteoporosis, and cancer. Since discovered in 1940, carbonic anhydrase Ⅱ has been an important drug target with more attention. Up to now, many inhibitors were discovered including some clinical therapeutic drugs. This paper reviewed recent developments in structures, functions and inhibitors of human carbonic anhydrase Ⅱ.

Key words: Carbonic Anhydrase Ⅱ

摘要： 碳酸酐酶Ⅱ是一种活性中心含有Zn²⁺ 、能催化CO_² + H₂O\ HCO₃^- + H⁺ 反应的金属酶。它广泛分布于人体多种组织、器官中, 与人体酸碱平衡、青光眼、骨质疏松症、癌症等多种生理或病理过程密切相关, 多年来一直备受关注。自从1992 年高分辨率的碳酸酐酶Ⅱ 晶体结构测定以来, 其抑制剂研究发展较快, 已有活性好、选择性强的抑制剂作为新药应用于临床。本文以碳酸酐酶Ⅱ结构、功能和抑制剂研究为重点, 主要介绍近15 年来该领域研究的一些重要进展。

关键词: 碳酸酐酶Ⅱ, 结构, 功能, 抑制剂FONT