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基于组蛋白去乙酰化酶的双靶点抑制剂研究进展
石安喆,武善超,盛春泉*
0
(海军军医大学(第二军医大学)药学系药物化学教研室, 上海 200433
*通信作者)
摘要:
组蛋白去乙酰化酶(HDAC)是肿瘤治疗中的重要靶标,目前已有多个HDAC抑制剂类药物被批准应用于临床。相对于单靶点药物,多靶点药物具有更好的药效和特异性,能够有效提高疗效、降低耐药性,在阿尔茨海默病、真菌病、肿瘤等疾病的治疗中具有较大开发前景。本文主要介绍抗阿尔茨海默病、抗真菌、抗肿瘤领域基于HDAC设计的双靶点抑制剂的研究进展,为该类药物的研发和应用提供参考。
关键词:  组蛋白脱乙酰基酶类  双靶点抑制剂  阿尔茨海默病  真菌病  肿瘤
DOI:10.16781/j.0258-879x.2021.05.0543
投稿时间:2021-04-09修订日期:2021-05-11
基金项目:国家自然科学基金青年科学基金(21807113).
Dual-target inhibitors based on histone deacetylase: research progress
SHI An-zhe,WU Shan-chao,SHENG Chun-quan*
(Department of Medicinal Chemistry, School of Pharmacy, Naval Medical University(Second Military Medical University), Shanghai 200433, China
*Corresponding author)
Abstract:
Histone deacetylase (HDAC) is an important target in cancer treatment, and several HDAC inhibitors have been approved for clinical treatment. Compared with single-target drugs, multi-target drugs have better drug efficacy and specificity, can effectively improve the efficacy and reduce the drug resistance, and have great prospects for the treatment of Alzheimer's disease, mycosis, tumor and other diseases. This article mainly introduces the research progress of HDAC dual-target inhibitors in anti-Alzheimer's disease, anti-fungi and anti-tumor fields, so as to provide reference for the development and application of the drugs.
Key words:  histone deacetylases  dual-target inhibitor  Alzheimer disease  mycosis  neoplasms