Design and Synthesis of a Novel Peptidomimetic Inhibitor of Caspase-3

作     者：ZHANG Jin-liang LIU Lin-hua GUO Yang-hong YANG Jin-gang LI Wei ZHONG Da-fang WANG Ji-dong 

作者机构：College of Life Science Jilin University Changchun 130021 P. R. China 

基　　金：SupportedbytheNationalNaturalScienceFoundationofChina(No.30371675)andtheFoundationofScience&TechnologyDepartmentofJilinProvince(No.20040543) 

出 版 物：《Chemical Research in Chinese Universities》 (高等学校化学研究（英文版）)

年 卷 期：2006年第22卷第2期

页      码：225-228页

摘      要：Caspases, a family of cysteine proteases, comprise of highly homologous enzymes that play an important role in apoptotic cell death. Caspase-3 shows key functions in apoptosis, mediating apoptotic cascade from the intrinsic and extrinsic activation pathways. Therefore, caspase-3 is an attractive target for therapeutic intervention. For instance, inhibitors of caspase-3 have been described as promising cardioprotectants, neuroprotectants and antiarthritic agents. A novel peptidomimetic inhibitor of caspase-3, has been designed, which still has the properties of a reversible inhibitor, while the P1 site at the C-terminal remains, and only L-amino acid has been replaced by D-amino acid. Also presented here is the synthesis of the inhibitor and its inhibitory activity against caspase-3, which was tested by the fluorescent activity assay.

主 题 词：Caspase-3 Inhibitor Retro-inverso Peptidomimetie Synthesis 

学科分类：0710[理学-生物科学类] 071010[071010] 081704[081704] 07[理学] 08[工学] 0817[工学-轻工类] 

核心收录：

D　O　I：10.1016/S1005-9040(06)60082-2

馆 藏 号：203217438...