摘要
热休克蛋白90(Hsp90)是抗肿瘤药物作用的新靶点,其抑制剂通过破坏体内蛋白的结构和降解过程起到抗肿瘤的作用。近年来,Hsp90抑制剂的研究不仅拘泥于对天然产物的结构改造,更多的是通过高通量筛选和计算机辅助药物设计方法进行先导化合物的发现以及合成新型结构的Hsp90抑制剂。Hsp90作为一类重要的生物学靶点在抗肿瘤药物的研制过程中越来越受到重视。本文对近年来以Hsp90为靶点的小分子抑制剂的研究进展进行综述。
Heat shock protein 90 is a new target of antitumor drug,the inhibitor of Hsp90 fight against tumor by destroy and degrade the structure of protein.In recent years,looking for Hsp90 inhibitor is not only via structure modifying of natural products,but also via high throughput screening and computer aided drug design to find and synthesize new kinds of Hsp90 inhibitor.Anyway,Hsp90 inhibitor has considered as an important biology target and to pay more and more attention.This review describes recent developments of small molecule Hsp90 inhibitors.
出处
《药学学报》
CAS
CSCD
北大核心
2010年第7期813-820,共8页
Acta Pharmaceutica Sinica
关键词
热休克蛋白90抑制剂
高通量筛选
构效关系
分子-蛋白复合物
进展
heat shock protein 90 inhibitor
high throughput screening
structure activity relationship
molecule-protein complex
progress