环肽类组蛋白去乙酰化酶抑制剂研究进展

Advances in Research on Cyclic Peptide Histone Deacetylase Inhibitors

组蛋白去乙酰化酶是一类对染色体结构修饰和基因表达调控具有重要作用的蛋白酶,其异常活化与肿瘤的发生、发展密切相关。抑制组蛋白去乙酰化酶活性已成为抗肿瘤治疗的有效策略之一。对组蛋白去乙酰化酶抑制剂的抗肿瘤作用机制进行介绍,并重点综述环肽类组蛋白去乙酰化酶抑制剂的研究进展,旨在为该类药物的深入开发提供参考。

Histone deacetylase （HDAC） is a kind of protease that plays an important role in chromo- some structural modification and gene expression regulation. The abnormal activation of HDAC is closely related to generation and progression of cancer. Inhibition of HDAC activity has become an effective anti- tumor therapeutic strategy. The anti-tumor mechanisms of HDAC inhibitors （HDACIs） have been intro- duced in this paper. Moreover, the research progresses in cyclic peptides HDACIs have been especially reviewed in this paper, in order to provide references for the further development of this kind of drugs.