Χa因子抑制剂的研究进展  

Advances in the research of factor Xa inhibitors

作　　者：陈鑫[1] 张惠斌[1] 黄文龙[1] 江凯[1] 

机构地区：[1]中国药科大学新药研究中心,南京210009

出　　处：《中国药科大学学报》2010年第2期104-111,共8页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.30973638);国家“重大新药创制”科技重大专项资助项目(No.2009ZX09103-094)~~

摘　　要：Χa因子是一种丝氨酸蛋白酶,在凝血过程中起关键作用,是临床上预防和治疗凝血的新靶点,在口服抗凝剂的开发中扮演着重要角色,近年来引起药学工作者的广泛关注。本文综述了几类主要的直接Χa因子抑制剂及其构效关系的最新研究进展,特别是利用现有抑制剂-酶复合物晶体X-衍射研究得到的Χa因子结合位点的重要结构信息,从结构上进一步分析Χa因子与多种不同类型的药物分子相结合的作用机制,从而总结出抑制剂-酶紧密结合的重要分子间相互作用,为基于结构的药物设计以获得新型Χa因子抑制剂提供较好的理论依据。Factor Xa is a trypsin-like serine protease playing a pivotal role in the blood coagulation cascade.Factor Xa and its inhibitors are of great importance in the development of orally active antithrombotic agents and have aroused considerable attention from the pharmaceutical industry sector over the years.In this review,the structural characteristics of the factor Xa binding site are discussed and the X-ray information available together with the published structure-activity relationship data is used to identify the molecular interactions that are most important for tight enzymeinhibitor binding,which would be useful in the structurebased drug design of novel factor Xa inhibitors.

关 键 词：XA因子抑制剂 构效关系 研究进展 

分 类 号：R96[医药卫生—药理学]