MRC Human Reproductive Sciences Unit, Queen's Medical Research Institute, 47 Little France Crescent, Edinburgh EH16 4TJ, Scotland, UK.
Reproduction. 2010 Jul;140(1):93-104. doi: 10.1530/REP-10-0140. Epub 2010 Apr 20.
The androgen receptor (AR) is a member of the nuclear receptor superfamily, and is important for both male and female reproductive health. The receptor is a target for a number of post-translational modifications including phosphorylation, which has been intensively studied in vitro. However, little is known about the phosphorylation status of the receptor in target tissues in vivo. The common marmoset is a useful model for studying human reproductive functions, and comparison of the AR primary sequence from this primate shows high conservation of serines known to be phosphorylated in the human receptor and corresponding flanking amino acids. We have used a panel of phosphospecific antibodies to study AR phosphorylation in the marmoset ovary throughout the follicular phase and after treatment with GNRH antagonist or testosterone propionate. In normal follicular phase ovaries, total AR (both phosphorylated and non-phosphorylated forms) immunopositive staining was observed in several cell types including granulosa cells of developing follicles, theca cells and endothelial cells lining blood vessels. Receptor phosphorylation at serines 81, 308, and 650 was detected primarily in the granulosa cells of developing follicles, surface epithelium, and vessel endothelial cells. Testosterone treatment lead to a modest increase in AR staining in all stages of follicle studied, while GNRH antagonist had no effect. Neither treatment significantly altered the pattern of phosphorylation compared to the control group. These results demonstrate that phosphorylation of the AR occurs, at a subset of serine residues, in a reproductive target tissue in vivo, which appears refractory to hormonal manipulations.
雄激素受体(AR)是核受体超家族的成员,对男性和女性的生殖健康都很重要。该受体是许多翻译后修饰的靶点,包括磷酸化,这在体外已经得到了深入研究。然而,关于受体在体内靶组织中的磷酸化状态知之甚少。普通狨猴是研究人类生殖功能的有用模型,与该灵长类动物的 AR 一级序列比较表明,其丝氨酸的磷酸化状态与人类受体中已知的磷酸化位点以及相应的侧翼氨基酸高度保守。我们使用一组磷酸特异性抗体来研究 GnRH 拮抗剂或丙酸睾酮处理后普通狨猴卵巢在整个卵泡期和卵泡期后的 AR 磷酸化。在正常的卵泡期卵巢中,几种细胞类型包括发育中的卵泡的颗粒细胞、卵泡膜细胞和血管内皮细胞中观察到总 AR(磷酸化和非磷酸化形式)免疫阳性染色。在发育中的卵泡的颗粒细胞、表面上皮细胞和血管内皮细胞中,检测到 AR 丝氨酸 81、308 和 650 的磷酸化。睾酮处理导致研究的所有卵泡阶段的 AR 染色略有增加,而 GnRH 拮抗剂则没有影响。与对照组相比,两种处理都没有明显改变磷酸化模式。这些结果表明,AR 的磷酸化在体内生殖靶组织中发生,在一组丝氨酸残基上,这似乎对激素处理有抗性。