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

高等学校化学研究 ›› 2006, Vol. 22 ›› Issue (2): 225-228.

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

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

College of Life Science, Jilin University, Changchun 130021, P.R.China

收稿日期:2005-12-20 出版日期:2006-04-24 发布日期:2011-08-06
基金资助:
Supported by the National Natural Science Foundation of China(No.30371675) and the Foundation of Science & Technology Department of Jilin Province(No.20040543).

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

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

College of Life Science, Jilin University, Changchun 130021, P.R.China

Received:2005-12-20 Online:2006-04-24 Published:2011-08-06
Supported by:
Supported by the National Natural Science Foundation of China(No.30371675) and the Foundation of Science & Technology Department of Jilin Province(No.20040543).

摘要/Abstract

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has the properties of a reversible inhibitor, while the P1 site at the C-terminal remains, and only L-amino acid has been replaced by D-amino acid.Also presented here is the synthesis of the inhibitor and its inhibitory activity against caspase-3, which was tested by the fluorescent activity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.

关键词: Caspase-3, Inhibitor, Retro-inverso, Peptidomimetic, Synthesis

Abstract: 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.

Key words: Caspase-3, Inhibitor, Retro-inverso, Peptidomimetic, Synthesis

ZHANG Jin-liang, LIU Lin-hua, GUO Yang-hong, YANG Jin-gang, LI Wei, ZHONG Da-fang, WANG Ji-dong. Design and Synthesis of a Novel Peptidomimetic Inhibitor of Caspase-3[J]. 高等学校化学研究, 2006, 22(2): 225-228.

ZHANG Jin-liang, LIU Lin-hua, GUO Yang-hong, YANG Jin-gang, LI Wei, ZHONG Da-fang, WANG Ji-dong. Design and Synthesis of a Novel Peptidomimetic Inhibitor of Caspase-3[J]. Chemical Research in Chinese Universities, 2006, 22(2): 225-228.

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

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

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