Deng Changhui, Ueda Eric, Chen Kuanhui E, Bula Craig, Norman Anthony W, Luben Richard A, Walker Ameae M
Division of Biomedical Sciences, University of California, Riverside, California 92521, USA.
Mol Endocrinol. 2009 Feb;23(2):226-36. doi: 10.1210/me.2008-0075. Epub 2008 Dec 12.
Based on their content of prolactin receptors, osteosarcoma cells were predicted to be responsive to prolactin (PRL), but whether PRL would be beneficial or contribute to pathogenesis was unclear. 1,25(OH)(2) vitamin D(3) [1alpha,25(OH)(2)D(3)] has antiproliferative effects on osteosarcoma cells, and a complex interregulatory situation exists between PRL and 1alpha,25(OH)(2)D(3). Using osteosarcoma cells, Western blot, real time RT-PCR, and promoter-luciferase assays, we have examined the interaction between PRL and 1alpha,25(OH)(2)D(3) and demonstrated that physiological concentrations of PRL block increased osteocalcin and vitamin D receptor (VDR) expression in response to 1alpha,25(OH)(2)D(3.) This blockade was shown to be the result of lack of nuclear accumulation of the VDR in response to 1alpha,25(OH)(2)D(3). Although inhibition of proteasomic degradation with MG132 had no effect on the VDR itself in a 30-min time frame, it relieved the blockade by PRL. Analysis of ubiquitinated proteins brought down by immunoprecipitation with anti-VDR showed PRL regulation of a 250-kDa protein-VDR complex. P250 was identified as the breast cancer tumor suppressor gene product, BRCA1, by Western blot of the VDR immunoprecipitate and confirmed by immunoprecipitation with anti-BRCA1 and blotting for the VDR in the absence and presence of PRL. Knockdown of BRCA1 inhibited nuclear translocation of the VDR and the ability of 1alpha,25(OH)(2)D(3) to induce the VDR. This, to our knowledge, is the first demonstration of a role for BRCA1 in nuclear accumulation of a steroid hormone and the first demonstration that PRL has the potential to affect the cell cycle through effects on BRCA1.
基于其催乳素受体的含量,骨肉瘤细胞被预测对催乳素(PRL)有反应,但PRL是有益还是会促进发病机制尚不清楚。1,25(OH)₂维生素D₃[1α,25(OH)₂D₃]对骨肉瘤细胞有抗增殖作用,并且PRL与1α,25(OH)₂D₃之间存在复杂的相互调节情况。利用骨肉瘤细胞、蛋白质免疫印迹法、实时逆转录-聚合酶链反应以及启动子-荧光素酶分析,我们研究了PRL与1α,25(OH)₂D₃之间的相互作用,并证明生理浓度的PRL会阻断1α,25(OH)₂D₃诱导的骨钙素和维生素D受体(VDR)表达增加。这种阻断被证明是由于VDR在响应1α,25(OH)₂D₃时缺乏核积累所致。尽管在30分钟的时间范围内用MG132抑制蛋白酶体降解对VDR本身没有影响,但它缓解了PRL的阻断作用。用抗VDR免疫沉淀法沉淀的泛素化蛋白分析显示PRL对一种250 kDa蛋白-VDR复合物有调节作用。通过对VDR免疫沉淀物进行蛋白质免疫印迹法鉴定P250为乳腺癌肿瘤抑制基因产物BRCA1,并通过用抗BRCA1免疫沉淀以及在有无PRL的情况下对VDR进行印迹分析加以证实。敲低BRCA1会抑制VDR的核转位以及1α,25(OH)₂D₃诱导VDR的能力。据我们所知,这是首次证明BRCA1在类固醇激素核积累中的作用,也是首次证明PRL有可能通过影响BRCA1来影响细胞周期。