Matulis Christina K, Mayo Kelly E
Department of Molecular Biosciences and Center of Reproductive Science, Northwestern University, Evanston, Illinois 60208, USA.
Mol Endocrinol. 2012 Aug;26(8):1278-90. doi: 10.1210/me.2011-1347. Epub 2012 Jun 25.
Nuclear receptor transcriptional activity is enhanced by interaction with coactivators. The highly related nuclear receptor 5A (NR5A) subfamily members liver receptor homolog 1 and steroidogenic factor 1 bind to and activate several of the same genes, many of which are important for reproductive function. To better understand transcriptional activation by these nuclear receptors, we sought to identify interacting proteins that might function as coactivators. The LIM domain protein four and a half LIM domain 2 (FHL2) was identified as interacting with the NR5A receptors in a yeast two-hybrid screen of a human ovary cDNA library. FHL2, and the closely related FHL1, are both expressed in the rodent ovary and in granulosa cells. Small interfering RNA-mediated knockdown of FHL1 and FHL2 in primary mouse granulosa cells reduced expression of the NR5A target genes encoding inhibin-α and P450scc. In vitro assays confirmed the interaction between the FHL and NR5A proteins and revealed that a single LIM domain of FHL2 is sufficient for this interaction, whereas determinants in both the ligand binding domain and DNA binding domain of NR5A proteins are important. FHL2 enhances the ability of both liver receptor homolog 1 and steroidogenic factor 1 to activate the inhibin-α subunit gene promoter in granulosa cells and thus functions as a transcriptional coactivator. FHL2 also interacts with cAMP response element-binding protein and substantially augments activation of inhibin gene expression by the combination of NR5A receptors and forskolin, suggesting that FHL2 may facilitate integration of these two signals. Collectively these results identify FHL2 as a novel coactivator of NR5A nuclear receptors in ovarian granulosa cells and suggest its involvement in regulating target genes important for mammalian reproduction.
核受体转录活性通过与共激活因子相互作用而增强。高度相关的核受体5A(NR5A)亚家族成员肝受体同源物1和类固醇生成因子1与几个相同的基因结合并激活它们,其中许多基因对生殖功能很重要。为了更好地理解这些核受体的转录激活作用,我们试图鉴定可能作为共激活因子发挥作用的相互作用蛋白。在人卵巢cDNA文库的酵母双杂交筛选中,LIM结构域蛋白四半LIM结构域2(FHL2)被鉴定为与NR5A受体相互作用。FHL2以及与之密切相关的FHL1在啮齿动物卵巢和颗粒细胞中均有表达。在原代小鼠颗粒细胞中,小干扰RNA介导的FHL1和FHL2敲低降低了编码抑制素-α和P450scc的NR5A靶基因的表达。体外试验证实了FHL与NR5A蛋白之间的相互作用,并表明FHL2的单个LIM结构域足以实现这种相互作用,而NR5A蛋白的配体结合结构域和DNA结合结构域中的决定因素都很重要。FHL2增强了肝受体同源物1和类固醇生成因子1在颗粒细胞中激活抑制素-α亚基基因启动子的能力,因此作为转录共激活因子发挥作用。FHL2还与cAMP反应元件结合蛋白相互作用,并通过NR5A受体和福斯可林的组合显著增强抑制素基因表达的激活,这表明FHL2可能促进这两种信号整合。这些结果共同确定FHL2为卵巢颗粒细胞中NR5A核受体的新型共激活因子,并表明其参与调节对哺乳动物生殖重要的靶基因。