Zhang Yanping, Knutsen Gregory R, Brown Matthew D, Ruest L Bruno
Center for Craniofacial Research and Diagnosis and Department of Biomedical Sciences, Texas A&M University-Baylor College of Dentistry, Dallas, Texas 75246, USA.
Mol Endocrinol. 2013 Jun;27(6):892-908. doi: 10.1210/me.2012-1334. Epub 2013 Apr 16.
The endothelin-A receptor (Ednra) is involved in several physiological, pathological, and developmental pathways. Known for its function in vasoconstriction after being activated by endothelin-1, Ednra also controls cephalic neural crest cell development and appears to play a role in several pathologies, including cancer and periodontitis. However, the mechanisms regulating Ednra expression have not been identified despite its important functions. In this study, we investigated the role progesterone plays in Ednra gene expression in vivo and in vitro. In mice, pregnancy promotes Ednra expression in the heart, kidney, lung, uterus, and placenta, and the up-regulation is mediated by progesterone. We determined that the conserved region between -5.7 and -4.2 kb upstream of the mouse Ednra gene is necessary for the progesterone response. We also found that progesterone mediates Ednra activation through progesterone receptor B activation by its recruitment to PRE6, one of the 6 progesterone response elements found in that locus. However, gene activation by means of a GATA2 site was also necessary for the progesterone response. The Gata2 transcription factor enhances the progesterone response mediated by the progesterone receptor B. Together these results indicate that progesterone regulates Ednra expression by synergizing with Gata2 activity, a previously unknown mechanism. This mechanism may have an impact on pathologies involving the endothelin signaling.
内皮素-A受体(Ednra)参与多种生理、病理和发育途径。Ednra在被内皮素-1激活后具有血管收缩功能,它还控制头部神经嵴细胞的发育,并且似乎在包括癌症和牙周炎在内的多种病理过程中发挥作用。然而,尽管Ednra具有重要功能,但其表达调控机制尚未明确。在本研究中,我们调查了孕酮在体内和体外对Ednra基因表达的作用。在小鼠中,怀孕会促进心脏、肾脏、肺、子宫和胎盘中Ednra的表达,且这种上调是由孕酮介导的。我们确定小鼠Ednra基因上游-5.7至-4.2 kb之间的保守区域对于孕酮反应是必需的。我们还发现,孕酮通过招募到该位点发现的6个孕酮反应元件之一的PRE6来激活孕酮受体B,从而介导Ednra的激活。然而,通过GATA2位点进行基因激活对于孕酮反应也是必需的。Gata2转录因子增强了孕酮受体B介导的孕酮反应。这些结果共同表明,孕酮通过与Gata2活性协同作用来调节Ednra表达,这是一种此前未知的机制。该机制可能会对涉及内皮素信号传导的病理过程产生影响。