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引用本文:黄亚天,陆涛.作用于多靶点的组蛋白去乙酰化酶抑制剂结构设计的研究进展[J].中国现代应用药学,2013,30(9):1037-1042.
HUANG Yatian,LU Tao.Progress in the Research of Structural Design in Multi-targeted Histone Deacetylase Inhibitors[J].Chin J Mod Appl Pharm(中国现代应用药学),2013,30(9):1037-1042.
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作用于多靶点的组蛋白去乙酰化酶抑制剂结构设计的研究进展
黄亚天, 陆涛
中国药科大学有机化学教研室,南京 210009
摘要:
目的 肿瘤产生机制的复杂性,要求对多种促肿瘤发生发展机制同时抑制,才能有效阻止肿瘤生长。组蛋白去乙酰化酶抑制剂(HDACi)作为一种新型抗肿瘤药物,能诱导肿瘤细胞凋亡, 阻止癌细胞增长。利用结构的多样性和变通性设计新颖的作用于多靶点的HDACi。方法 分类总结大量已被报道的多靶点组蛋白去乙酰化酶抑制剂。结果 多靶点抑制剂在临床实验中表现出了较好的抗肿瘤活性。结论 多靶点单一分子的HDACi的研究日益引起人们的重视,具有广阔的研发前景。
关键词:  组蛋白去乙酰化酶抑制剂  多靶点抑制剂  抗肿瘤  研究进展
DOI:
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基金项目:
Progress in the Research of Structural Design in Multi-targeted Histone Deacetylase Inhibitors
HUANG Yatian, LU Tao
Organic Chemistry Staffroom, China Pharmaceutical University, Nanjing 210009, China
Abstract:
OBJECTIVE The heterogeneous nature of cancer requires a comprehensive approach for attacking the multiple mechanisms underlying the initiation and progression of cancer. HDACi have emerged as a new class of anticancer agents, targeting the biological processes including cell cycle, apoptosis and differentiation. Design novel multi-target HDACi based on the structural diversity and adaptation. METHODS Classify and summarize large numbers of reported multi-target histone deacetylase inhibitors. RESULTS Multi-target inhibitors in clinical trials show good antitumor activity. CONCLUSION Multi-target single-molecule HDAC inhibitors have attracted much attention, and have broad prospects for development.
Key words:  HDACi  multi-targeted inhibitor  cancer therapy  research development
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