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组蛋白脱乙酰基酶是一类锌离子依赖性的金属蛋白酶。它们参与染色体结构的修饰和改造,调节基因转录以及肿瘤抑制因子p53、热休克蛋白90和α-微管蛋白等一些重要蛋白质和细胞因子的活性,对肿瘤发生起到关键作用,是近年来抗肿瘤药物设计的新靶点。组蛋白去乙酰化酶抑制剂(HDACi)能有效抑制癌细胞的增殖,诱导细胞凋亡,一些在体内和体外活性较好的HDACi已进入临床试验。本文综述了目前在临床研究中的HDACi的结构特点、活性评价和治疗作用。
Histone deacetylase is a type of zinc ion-dependent metalloproteinase. They are involved in the modification and modification of chromosomal structure, regulating gene transcription and the activities of some important proteins and cytokines such as tumor suppressor p53, heat shock protein 90 and α-tubulin, which play a key role in tumorigenesis and have been used in recent years New target for oncology drug design. Histone deacetylase inhibitors (HDACi) can effectively inhibit the proliferation of cancer cells and induce apoptosis. Some of the HDACi active in vivo and in vitro have been put into clinical trials. This review summarizes the structural features, activity evaluation and therapeutic effects of HDACi in clinical studies.