精子顶体反应与抗生育小分子化合物研究进展

Acrosome reaction and anti-fertility small molecule compounds

顶体蛋白酶是存在于所有哺乳动物精子顶体中的一种胰蛋白酶样的蛋白水解酶,它参与精卵结合并能溶解透明带。这种功能的实现是通过识别同源性透明带糖蛋白和在顶体反应时调节顶体内容物的释放。对于精子顶体反应的研究有助于了解受精过程并人为进行控制与干预并开发男性避孕剂。文中通过对国内外顶体酶小分子抑制剂的研究和开发状况进行分析和总结,为寻找高效低毒的男性抗生育先导化合物提供参考。

Acrosin, a trypsin-like endoprotease, presents in the aerosome of all mammalian spermatozoa studied. It has been involved in sperm-egg interaction by participating in the proteolysis of the zona pellueida （ZP） , by regulating the release of acrosomal components during the acrosome reaction, and by recognizing homologous ZP glycoproteins. The sperm aerosome reaction research helps us to understand and control the process of fertilization, and develop new male contraceptive agents. By analyzing and summarizing research and development status of the small molecule inhibitors of acrosomal enzyme at home and abroad, we put forward searching high efficient and low toxicity male anti fertility drugs.