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 

机构地区：[1]College of Life Science, Jilin University, Changchun 130021, P. R. China

出　　处：《Chemical Research in Chinese Universities》2006年第2期225-228,共4页高等学校化学研究（英文版）

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

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has the properties of a reversible inhibitor, while the P1 site at the C-terminal remains, and only L-amino acid has been replaced by D-amino acid.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.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has the properties of a reversible inhibitor, while the P1 site at the C-terminal remains, and only L-amino acid has been replaced by D-amino acid.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.

关 键 词：CASPASE-3 INHIBITOR Retro-inverso Peptidomimetie SYNTHESIS 

分 类 号：Q55[生物学—生物化学]