Department of Pharmacology and Therapeutics, Centre for Research in Reproduction and Development, McGill University, Montreal, Quebec, Canada.
J Mol Endocrinol. 2019 Feb 1;62(2):67-78. doi: 10.1530/JME-18-0145.
Fertility is dependent on follicle-stimulating hormone (FSH), a product of gonadotrope cells of the anterior pituitary gland. Hypothalamic gonadotropin-releasing hormone (GnRH) and intra-pituitary activins are regarded as the primary drivers of FSH synthesis and secretion. Both stimulate expression of the FSH beta subunit gene (Fshb), although the underlying mechanisms of GnRH action are poorly described relative to those of the activins. There is currently no consensus on how GnRH regulates Fshb transcription, as results vary across species and between in vivo and in vitro approaches. One of the more fully developed models suggests that the murine Fshb promoter is tonically repressed by histone deacetylases (HDACs) and that GnRH relieves this repression, at least in immortalized murine gonadotrope-like cells (LβT2 and αT3-1). In contrast, we observed that the class I/II HDAC inhibitor trichostatin A (TSA) robustly inhibited basal, activin A-, and GnRH-induced Fshb mRNA expression in LβT2 cells and in primary murine pituitary cultures. Similar results were obtained with the class I specific HDAC inhibitor, entinostat, whereas two class II-specific inhibitors, MC1568 and TMP269, had no effects on Fshb expression. Collectively, these data suggest that class I HDACs are positive, not negative, regulators of Fshb expression in vitro and that, contrary to earlier reports, GnRH may not stimulate Fshb by inhibiting HDAC-mediated repression of the gene.
生育能力取决于卵泡刺激素 (FSH),它是垂体前叶促性腺细胞的产物。下丘脑促性腺激素释放激素 (GnRH) 和脑垂体激活素被认为是 FSH 合成和分泌的主要驱动因素。两者都刺激 FSHβ亚基基因 (Fshb) 的表达,尽管 GnRH 作用的潜在机制相对于激活素的作用机制描述得较差。目前对于 GnRH 如何调节 Fshb 转录没有共识,因为结果因物种而异,并且在体内和体外方法之间也存在差异。一个更成熟的模型表明,小鼠 Fshb 启动子被组蛋白去乙酰化酶 (HDACs) 持续抑制,而 GnRH 至少在永生化的小鼠促性腺激素样细胞 (LβT2 和 αT3-1) 中解除这种抑制。相比之下,我们观察到 I 类/II 类 HDAC 抑制剂曲古抑菌素 A (TSA) 可强烈抑制 LβT2 细胞和原代小鼠垂体培养物中基础、激活素 A 和 GnRH 诱导的 Fshb mRNA 表达。I 类特异性 HDAC 抑制剂恩替诺特也得到了类似的结果,而两种 II 类特异性抑制剂 MC1568 和 TMP269 对 Fshb 表达没有影响。总的来说,这些数据表明,I 类 HDAC 是体外 Fshb 表达的正向而非负向调节剂,并且与早期报告相反,GnRH 可能不是通过抑制基因的 HDAC 介导的抑制来刺激 Fshb。