首页|基于组蛋白去乙酰化酶6设计的抗肿瘤抑制剂研究进展

基于组蛋白去乙酰化酶6设计的抗肿瘤抑制剂研究进展

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组蛋白去乙酰化酶6(HDAC6)是组蛋白去乙酰化酶家族成员,除了可以调控组蛋白的乙酰化状态外,还能催化多种非组蛋白底物,如α-tubulin、cortactin、HSP90、HSF-1、Ku-70和PD-L1等,这些非组蛋白底物在肿瘤的发生发展过程中起到重要作用,因此,HDAC6已成为抗肿瘤药物研发的潜在靶点.本文作者对近年来HDAC6抑制剂的研究进展进行综述,并根据化合物结构进行归纳和总结,以期为后续研究提供思路与方向.
Research progress in antitumor inhibitors based on histone deacetylase 6
Histone deacetylase 6(HDAC6)is a member of the histone deacetylase family,which not only regulates the acetylation state of histones,but also catalyzes various nonhistone substrates,includingα-tubulin,cortactin,HSP90,HSF-1,Ku-70,and PD-L1.These substrates play important roles in the occurrence and development of tumors.Therefore,HDAC6 has become a potential target for the development of antitumor drugs.In this paper,the research progress in antitumor inhibitors based on histone deacetylase 6 was introduced,and the compounds on the basis of structure in recent years were summarized.This review will provide ideas and directions for the further research.

histone deacetylase 6small molecule inhibitorantitumor drug

谢昭、王瑞、陈瀚、王岩石

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朴创医药科技(天津)有限公司,天津 300301

天津药物研究院药物成药性评价与系统性转化全国重点实验室,天津 300301

天津药物研究院天津市新药设计与发现重点实验室,天津 300301

组蛋白去乙酰化酶6 小分子抑制剂 抗肿瘤药物

2024

中国药物化学杂志
沈阳药科大学,中国药学会

中国药物化学杂志

CSTPCD
影响因子:0.463
ISSN:1005-0108
年,卷(期):2024.34(3)