Freedman L P, Arce V, Perez Fernandez R
Cell Biology & Genetics Program Memorial Sloan-Kettering Cancer Center, New York, New York 10021.
Mol Endocrinol. 1994 Mar;8(3):265-73. doi: 10.1210/mend.8.3.8015545.
DNA binding site discrimination within a subgroup of nuclear receptors, including the human vitamin D3 receptor (hVDR), appears to be influenced primarily by spacing and orientation differences of response element half-sites, since many receptors recognize and bind to the same hexameric half-site sequence, AGGTCA. Small sequence differences within half-sites, however, may also play an important role in distinguishing between different receptor complexes. Several laboratories have reported that the AGGTCA element in a direct repeat (DR) configuration appears to be a high affinity recognition site for only nuclear receptor-9 retinoid X receptor (RXR) heterodimers. However, we have previously shown that a closely related, but distinct, element (AGTTCA; essentially the mouse osteopontin [Spp-1] vitamin D response element) acts as a high affinity target for purified hVDR in the absence of RXR. This suggests that some half-site sequences could be targets for hVDR alone while others serve as recognition elements for hVDR-RXR complexes. In this report, we test this hypothesis by selecting, using purified hVDR only, for high affinity receptor binding sites in a complex DNA mixture which should by chance contain such sequences. We find that the purified receptor selects a heptameric sequence resembling a half-site of the osteopontin vitamin D response element, consistent with osteopontin-like sequences acting as high affinity targets for hVDR in the absence of RXR. We directly test this by comparing the in vitro DNA binding activity of purified hVDR to DR+3 elements comprised of osteopontin-like AGTTCA or AGGTCA half-sites.(ABSTRACT TRUNCATED AT 250 WORDS)
在包括人类维生素D3受体(hVDR)在内的一组核受体中,DNA结合位点的识别似乎主要受反应元件半位点间距和方向差异的影响,因为许多受体识别并结合相同的六聚体半位点序列AGGTCA。然而,半位点内的小序列差异在区分不同受体复合物方面也可能起重要作用。几个实验室报告说,直接重复(DR)构型中的AGGTCA元件似乎只是核受体9-视黄酸X受体(RXR)异二聚体的高亲和力识别位点。然而,我们之前已经表明,一个密切相关但不同的元件(AGTTCA;本质上是小鼠骨桥蛋白[Spp-1]维生素D反应元件)在没有RXR的情况下作为纯化的hVDR的高亲和力靶点。这表明一些半位点序列可能仅是hVDR的靶点,而其他序列则作为hVDR-RXR复合物的识别元件。在本报告中,我们通过仅使用纯化的hVDR在复杂的DNA混合物中选择高亲和力受体结合位点来检验这一假设,该混合物应该偶然包含此类序列。我们发现纯化的受体选择了一个七聚体序列,类似于骨桥蛋白维生素D反应元件的半位点,这与骨桥蛋白样序列在没有RXR的情况下作为hVDR的高亲和力靶点一致。我们通过比较纯化的hVDR与由骨桥蛋白样AGTTCA或AGGTCA半位点组成的DR + 3元件的体外DNA结合活性来直接验证这一点。(摘要截短于250字)