Pikler G M, Webster R A, Spelsberg T C
Biochem J. 1976 May 15;156(2):399-408. doi: 10.1042/bj1560399.
Steroid hormones, including progesterone, are known to bind with high affinity (Kd approximately 1x10(-10)M) to receptor proteins once they enter target cells. This complex (the progesterone-receptor) then undergoes a temperature-and/or salt-dependent activation which allows it to migrate to the cell nucleus and to bind to the deoxyribonucleoproteins. The present studies demonstrate that binding the hormone-receptor complex in vitro to isolated nuclei from the oviducts of laying hens required the same conditions as do other studies of bbinding in vitro reported previously, e.g. the hormone must be complexed to intact and activated receptor. The assay of the nuclear binding by using multiple concentrations of progesterone receptor reveals the presence of more than one class of binding site in the oviduct nuclei. The affinity of each of these classes of binding sites range from Kd approximately 1x10(-9)-1x10(-8)M. Assays using free steroid (not complexed with receptor) show no binding to these sites. The binding to each of the classes of sites, displays a differential stability to increasing ionic concentrations, suggesting primarily an ionic-type interaction for all classes. Only the highest-affinity class of binding site is capable of binding progesterone receptor under physioligical-saline conditions. This class represent 6000-10000 sites per cell nucleus and resembles the sites detected in vivo (Spelsberg, 1976, Biochem. J. 156, 391-398) which cause maximal transcriptional response when saturated with the progesterone receptor. The multiple binding sites for the progesterone receptor either are not present or are found in limited numbers in the nuclei of non-target organs. Differences in extent of binding to the nuclear material between a target tissue (oviduct) and other tissues (spleen or erythrocyte) are markedly dependent on the ionic conditions, and are probably due to binding to different classes of sites in the nuclei.
类固醇激素,包括孕酮,一旦进入靶细胞,就会以高亲和力(解离常数Kd约为1×10⁻¹⁰M)与受体蛋白结合。这种复合物(孕酮 - 受体)随后会经历温度和/或盐依赖性激活,使其能够迁移到细胞核并与脱氧核糖核蛋白结合。目前的研究表明,在体外将激素 - 受体复合物与产蛋母鸡输卵管分离的细胞核结合,所需条件与之前报道的其他体外结合研究相同,例如激素必须与完整且活化的受体形成复合物。通过使用多种浓度的孕酮受体来测定核结合情况,结果显示输卵管细胞核中存在不止一类结合位点。这些类别的每个结合位点的亲和力范围为Kd约1×10⁻⁹ - 1×10⁻⁸M。使用游离类固醇(未与受体复合)的测定显示其不与这些位点结合。与各类位点的结合对增加的离子浓度表现出不同的稳定性,这表明所有类别主要是离子型相互作用。只有最高亲和力类别的结合位点能够在生理盐溶液条件下结合孕酮受体。这类位点每个细胞核有6000 - 10000个,类似于体内检测到的位点(斯佩尔斯伯格,1976年,《生物化学杂志》156卷,391 - 398页),当被孕酮受体饱和时会引起最大转录反应。孕酮受体的多个结合位点在非靶器官的细胞核中要么不存在,要么数量有限。靶组织(输卵管)与其他组织(脾脏或红细胞)在与核物质结合程度上的差异明显取决于离子条件,可能是由于与细胞核中不同类别的位点结合所致。