Esposito Gloria, Jaiswal Bijay S, Xie Fang, Krajnc-Franken Magda A M, Robben Tamara J A A, Strik Ankie M, Kuil Cor, Philipsen Ria L A, van Duin Marcel, Conti Marco, Gossen Jan A
Department of Pharmacology and Lead Discovery Unit, NV Organon, P.O. Box 20, 5340 BH, Oss, The Netherlands.
Proc Natl Acad Sci U S A. 2004 Mar 2;101(9):2993-8. doi: 10.1073/pnas.0400050101. Epub 2004 Feb 19.
To acquire the ability to fertilize, spermatozoa undergo complex, but at present poorly understood, activation processes. The intracellular rise of cAMP produced by the bicarbonate-dependent soluble adenylyl cyclase (sAC) has been suggested to play a central role in initiating the cascade of the events that culminates in spermatozoa maturation. Here, we show that targeted disruption of the sAC gene does not affect spermatogenesis but dramatically impairs sperm motility, leading to male sterility. sAC mutant spermatozoa are characterized by a total loss of forward motility and are unable to fertilize oocytes in vitro. Interestingly, motility in sAC mutant spermatozoa can be restored on cAMP loading, indicating that the motility defect observed is not caused by a structural defect. We, therefore, conclude that sAC plays an essential and nonredundant role in the activation of the signaling cascade controlling motility and, therefore, in fertility. The crucial role of sAC in fertility and the absence of any other obvious pathological abnormalities in sAC-deficient mice may provide a rationale for developing inhibitors that can be applied as a human male contraceptive.
为了获得受精能力,精子会经历复杂但目前仍知之甚少的激活过程。有人提出,由碳酸氢盐依赖性可溶性腺苷酸环化酶(sAC)产生的细胞内cAMP升高在启动最终导致精子成熟的一系列事件中起核心作用。在此,我们表明,靶向破坏sAC基因不会影响精子发生,但会显著损害精子活力,导致雄性不育。sAC突变体精子的特征是完全丧失向前运动能力,并且无法在体外使卵母细胞受精。有趣的是,sAC突变体精子的活力可以通过加载cAMP来恢复,这表明观察到的活力缺陷不是由结构缺陷引起的。因此,我们得出结论,sAC在控制活力的信号级联激活中起着必不可少且不可替代的作用,因此在生育能力方面也起着重要作用。sAC在生育能力中的关键作用以及sAC缺陷小鼠中没有任何其他明显的病理异常,可能为开发可作为人类男性避孕药的抑制剂提供理论依据。