Kinetics of inhibition of sperm β‐acrosin activity by suramin

FEBS Letters

Jones, Roy¹  Haines, Dianne S.²  Hermans, Josephine M.²  James, Peter S.¹ 

[1] Gamete Signalling Laboratory, The Babraham Institute, Cambridge CB2 4AT, UK;Department of Biochemistry and Molecular Biology, School of Pharmacy and Molecular Sciences, James Cook University, Townsville, Qld 4811, Australia

关键词: Spermatozoa;    β-Acrosin;    Fertilisation;    Suramin;    Serine protease;    Contraception;    ZP;    zona pellucida;   

DOI  :  10.1016/S0014-5793(03)00488-5

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Sperm β-acrosin activity is inhibited by suramin, a polysulfonated naphthylurea compound with therapeutic potential as a combined antifertility agent and microbicide. A kinetic analysis of enzyme inhibition suggests that three and four molecules of suramin bind to one molecule of ram and boar β-acrosins respectively. Surface charge distribution models of boar β-acrosin based on its crystal structure indicate several positively charged exosites that represent potential ‘docking’ regions for suramin. It is hypothesised that the spatial arrangement and distance between these exosites determines the capacity of β-acrosin to bind suramin.

【 授权许可】

Unknown