Webb P, Nguyen P, Shinsako J, Anderson C, Feng W, Nguyen M P, Chen D, Huang S M, Subramanian S, McKinerney E, Katzenellenbogen B S, Stallcup M R, Kushner P J
Metabolic Research Unit, University of California School of Medicine, San Francisco 94143-0540, USA.
Mol Endocrinol. 1998 Oct;12(10):1605-18. doi: 10.1210/mend.12.10.0185.
Estrogen receptor-alpha contains two transactivation functions, a weak constitutive activation function (AF-1) and a hormone-dependent activation function (AF-2). AF-2 works by recruiting a large coactivator complex, composed of one or more p160s, CREB-binding protein (CBP)/p300, and P/CAF (p300 and CBP-associated factor), via direct contacts with the p160s. We report here that independent AF-1 activity also requires p160 contacts. Unlike AF-2, which binds signature NR boxes in the center of the p160 molecule, AF-1 binds to sequences near the p160 C terminus. We propose that the ability of AF-1 and AF-2 to interact with separate surfaces of the same coactivator is important for the ability of these transactivation functions to synergize.
雌激素受体α包含两种反式激活功能,一种是弱组成型激活功能(AF-1),另一种是激素依赖性激活功能(AF-2)。AF-2通过与一种或多种p160、CREB结合蛋白(CBP)/p300和P/CAF(p300和CBP相关因子)组成的大型共激活因子复合物直接接触来发挥作用。我们在此报告,独立的AF-1活性也需要与p160接触。与结合在p160分子中心的标志性NR框的AF-2不同,AF-1与p160 C末端附近的序列结合。我们提出,AF-1和AF-2与同一共激活因子的不同表面相互作用的能力对于这些反式激活功能协同作用的能力很重要。