Caspase-3抑制剂研究进展  

Advances on inhibitors of Caspase-3

作　　者：张彦博[1] 程功[1] 钟国华[1] 

机构地区：[1]天然源农药与化学生物学教育部重点实验室,华南农业大学昆虫毒理研究室,广东广州510642

出　　处：《化学研究与应用》2009年第6期769-778,共10页Chemical Research and Application

基　　金：国家自然科学基金(30500335)项目资助;教育部全国优秀博士学位论文作者专项基金项目(2004061)资助

摘　　要：Caspase-3是细胞凋亡的关键酶和执行者,研究开发Caspase-3抑制剂对于阐明许多重要疾病,提供治疗方案以及开发新型农药、兽药都具有潜在应用价值。通过计算机辅助分子设计、高通量筛选等先进方法技术,近来国内外发现了许多类型各异的高活性Caspase-3抑制剂,不少化合物活性达到了纳摩尔级。本文从合成肽类抑制剂、合成非肽类抑制剂、天然肽类抑制剂、天然非肽类抑制剂角度对近年来国内外Caspase-3抑制剂研究进展进行了综述,旨在为相关研究提供参考。Caspase-3 is the essential component in the protease cascade reaction processes of cell apoptosis and the crucial enzyme and executive of apoptosis. Research and development of Caspase-3 inhibitor have potential applied value of elucidating the mechanism of many diseases of mammalian and providing treatment programme. By using high-tech methods such as computer-aid molecular design and high throughput screening, different types of Caspase-3 inhibitors have been developed, some of them show nanomolar potency. This paper summarizes advances of Caspase-3 inhibitor research at home and abroad in recent years from the perspective among synthesis peptide inhibitor, synthesis non-peptidic inhibitor, natural peptide inhibitor and natural non-peptidic inhibitor,which would provide valuable imformation for developing new inhibtiors of Caspases-3.

关 键 词：CASPASE-3 抑制剂 进展 

分 类 号：R914[医药卫生—药物化学]