Matsunaga Hideyuki, Sasaki Shigekazu, Suzuki Shingo, Matsushita Akio, Nakamura Hirotoshi, Nakamura Hiroko Misawa, Hirahara Naoko, Kuroda Go, Iwaki Hiroyuki, Ohba Kenji, Morita Hiroshi, Oki Yutaka, Suda Takafumi
Second Division, Department of Internal Medicine, Hamamatsu University School of Medicine, 1-20-1 Handayama, Higashi-ku, Hamamatsu, Shizuoka, 431-3192, Japan.
Kuma Hospital, 8-2-35 Shimoyamate-dori, Chuo-ku, Kobe, Hyogo, 650-0011, Japan.
PLoS One. 2015 Nov 16;10(11):e0142400. doi: 10.1371/journal.pone.0142400. eCollection 2015.
The inhibition of thyrotropin (thyroid stimulating hormone; TSH) by thyroid hormone (T3) and its receptor (TR) is the central mechanism of the hypothalamus-pituitary-thyroid axis. Two transcription factors, GATA2 and Pit-1, determine thyrotroph differentiation and maintain the expression of the β subunit of TSH (TSHβ). We previously reported that T3-dependent repression of the TSHβ gene is mediated by GATA2 but not by the reported negative T3-responsive element (nTRE). In thyrotrophs, T3 also represses mRNA of the type-2 deiodinase (D2) gene, where no nTRE has been identified. Here, the human D2 promoter fused to the CAT or modified Renilla luciferase gene was co-transfected with Pit-1 and/or GATA2 expression plasmids into cell lines including CV1 and thyrotroph-derived TαT1. GATA2 but not Pit-1 activated the D2 promoter. Two GATA responsive elements (GATA-REs) were identified close to cAMP responsive element. The protein kinase A activator, forskolin, synergistically enhanced GATA2-dependent activity. Gel-shift and chromatin immunoprecipitation assays with TαT1 cells indicated that GATA2 binds to these GATA-REs. T3 repressed the GATA2-induced activity of the D2 promoter in the presence of the pituitary-specific TR, TRβ2. The inhibition by T3-bound TRβ2 was dominant over the synergism between GATA2 and forskolin. The D2 promoter is also stimulated by GATA4, the major GATA in cardiomyocytes, and this activity was repressed by T3 in the presence of TRα1. These data indicate that the GATA-induced activity of the D2 promoter is suppressed by T3-bound TRs via a tethering mechanism, as in the case of the TSHβ gene.
甲状腺激素(T3)及其受体(TR)对促甲状腺激素(甲状腺刺激激素;TSH)的抑制作用是下丘脑 - 垂体 - 甲状腺轴的核心机制。两种转录因子,即GATA2和Pit-1,决定促甲状腺细胞的分化并维持TSHβ亚基(TSHβ)的表达。我们之前报道,TSHβ基因的T3依赖性抑制是由GATA2介导的,而非通过报道的负性T3反应元件(nTRE)。在促甲状腺细胞中,T3还抑制2型脱碘酶(D2)基因的mRNA,在该基因中尚未鉴定出nTRE。在此,将与CAT或修饰的海肾荧光素酶基因融合的人D2启动子与Pit-1和/或GATA2表达质粒共转染到包括CV1和促甲状腺细胞来源的TαT1在内的细胞系中。GATA2而非Pit-1激活了D2启动子。在靠近cAMP反应元件处鉴定出两个GATA反应元件(GATA-REs)。蛋白激酶A激活剂福司可林协同增强了GATA2依赖性活性。对TαT1细胞进行的凝胶迁移和染色质免疫沉淀分析表明,GATA2与这些GATA-REs结合。在垂体特异性TR即TRβ2存在的情况下,T3抑制了GATA2诱导的D2启动子活性。T3结合的TRβ2的抑制作用强于GATA2与福司可林之间的协同作用。D2启动子也受到心肌细胞中的主要GATA即GATA4的刺激,并且在TRα1存在的情况下,这种活性被T3抑制。这些数据表明,与TSHβ基因的情况一样,T3结合的TRs通过一种拴系机制抑制GATA诱导的D2启动子活性。