Div. of Renal Diseases and Hypertension, The Univ. of Texas Medical School at Houston, 6431 Fannin, MSB 5.124, Houston, TX 77030, USA.
Am J Physiol Renal Physiol. 2013 Sep 1;305(5):F653-62. doi: 10.1152/ajprenal.00177.2013. Epub 2013 Jun 26.
The epithelial Na+ channel (ENaC) in the distal nephron constitutes the rate-limiting step for renal sodium reabsorption. Aldosterone increases tubular sodium absorption in large part by increasing αENaC transcription in collecting duct principal cells. We previously reported that Af9 binds to +78/+92 of αENaC and recruits Dot1a to repress basal and aldosterone-sensitive αENaC transcription in mouse inner medullary collecting duct (mIMCD)3 cells. Despite this epigenetic repression, basal αENaC transcription is still evident and physiologically necessary, indicating basal operation of positive regulators. In the present study, we identified Sp1 as one such regulator. Gel shift and antibody competition assays using a +208/+240 probe revealed DNA-Sp1-containing complexes in mIMCD3 cells. Mutation of the +222/+229 element abrogated Sp1 binding in vitro and in promoter-reporter constructs stably expressed in mIMCD3 cells. Compared with the wild-type promoter, an αENaC promoter-luciferase construct with +222/+229 mutations exhibited much lower activity and impaired trans-activation in Sp1 overexpression experiments. Conversely, Sp1 knockdown inhibited endogenous αENaC mRNA and the activity of the wild-type αENaC promoter but not the mutated construct. Aldosterone triggered Sp1 recruitment to the αENaC promoter, which was required for maximal induction of αENaC promoter activity and was blocked by spironolactone. Sequential chromatin immunoprecipitation assays and functional tests of +78/+92 and +222/+229 αENaC promoter mutants indicated that while Sp1, Dot1a, and Af9 co-occupy the αENaC promoter, the Sp1 effects are functionally independent from Dot1a and Af9. In summary, Sp1 binding to a cis-element at +222/+229 represents the first identified constitutive driver of αENaC transcription, and it contributes to maximal aldosterone trans-activation of αENaC.
肾远曲小管中的上皮钠离子通道(ENaC)是肾脏钠重吸收的限速步骤。醛固酮通过增加集合管主细胞中αENaC 的转录,在很大程度上增加了管状钠离子的吸收。我们之前报道过,Af9 结合到 αENaC 的+78/+92 位并募集 Dot1a 来抑制小鼠内髓集合管(mIMCD)3 细胞中基础和醛固酮敏感的 αENaC 转录。尽管存在这种表观遗传抑制,但基础 αENaC 转录仍然明显存在且在生理上是必需的,这表明存在基础的正调控因子。在本研究中,我们鉴定了 Sp1 作为这样的一种调控因子。使用+208/+240 探针的凝胶迁移和抗体竞争实验显示 mIMCD3 细胞中存在 DNA-Sp1 结合复合物。体外和在 mIMCD3 细胞中稳定表达的启动子报告构建体中,+222/+229 元件的突变破坏了 Sp1 的结合。与野生型启动子相比,具有+222/+229 突变的 αENaC 启动子-荧光素酶构建体显示出低得多的活性,并且在 Sp1 过表达实验中转录激活受损。相反,Sp1 敲低抑制了内源性 αENaC mRNA 和野生型 αENaC 启动子的活性,但不抑制突变构建体。醛固酮触发 Sp1 募集到 αENaC 启动子,这是最大程度诱导 αENaC 启动子活性所必需的,并且被螺内酯阻断。连续的染色质免疫沉淀实验和+78/+92 和+222/+229 αENaC 启动子突变体的功能测试表明,虽然 Sp1、Dot1a 和 Af9 共同占据 αENaC 启动子,但 Sp1 的作用在功能上独立于 Dot1a 和 Af9。总之,Sp1 与+222/+229 处的顺式元件结合代表了鉴定的第一个基础驱动 αENaC 转录的因子,并且它有助于醛固酮对 αENaC 的最大转录激活。