Hormone-dependent coactivator binding to a hydrophobic cleft on nuclear receptors
Hormone-dependent coactivator binding to a hydrophobic cleft on nuclear receptors
复制标题
DOI：
10.1126/science.280.5370.1747
复制
发表时间：
1998-06-12
期刊：
影响因子：
56.9
通讯作者：
West, BL
中科院分区：
文献类型：
--
作者：
Feng, WJ;Ribeiro, RCJ;West, BL
核受体的配体结合结构域含有转录激活功能（AF-2），其介导辅激活蛋白的酶依赖性结合。对人甲状腺激素受体进行扫描表面诱变，以确定结合共激活因子糖皮质激素受体相互作用蛋白1（GRIP 1）和类固醇受体共激活因子1（SRC-1）的位点。转录的配体激活涉及通过将羧基末端的cr螺旋折叠到其他三个螺旋的支架上来形成该表面。这些特征可能代表了核受体的一般特征。
The ligand-binding domain of nuclear receptors contains a transcriptional activation function (AF-2) that mediates hormone-dependent binding of coactivator proteins. Scanning surface mutagenesis on the human thyroid hormone receptor was performed to define the site that binds the coactivators, glucocorticoid receptor-interacting protein 1 (GRIP1) and steroid receptor coactivator 1 (SRC-1), The residues involved encircle a small surface that contains a hydrophobic cleft. Ligand activation of transcription involves formation of this surface by folding the carboxyl-terminal cr helix against a scaffold of three other helices. These features may represent general ones for nuclear receptors.