Mechanistic studies to evaluate the enhanced antiproliferation of human keratinocytes by 1α,25-dihydroxyvitamin D3-3-bromoacetate, a covalent modifier of vitamin D receptor, compared to 1α,25-dihydroxyvitamin D3
Mechanistic studies to evaluate the enhanced antiproliferation of human keratinocytes by 1α,25-dihydroxyvitamin D3-3-bromoacetate, a covalent modifier of vitamin D receptor, compared to 1α,25-dihydroxyvitamin D3
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DOI：
10.1006/abbi.1999.1353
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发表时间：
1999-10-01
影响因子：
3.9
通讯作者：
Ray, R
中科院分区：
文献类型：
--
作者：
Chen, ML;Ray, S;Ray, R
1 α,25-二羟基维生素 D-3-3-溴乙酸酯 (1,25-(OH)(2)D-3-3-BE) 是 1 α,25-二羟基维生素 D-3 (1,25(OH)(2)D-3) 的亲和标记类似物，在 10(-10)- 时表现出比 1,25(OH)(2)D-3 更强的抗增殖活性培养的人角质形成细胞 (CHK) 中的 10(-6) M 剂量水平。此外，将细胞与 10(-6) M 1,25(OH)(2)D-3 预孵育，然后用不同剂量的 1,25(OH)(2)D-3-3-BE 处理，导致混合物在每个剂量水平上比单独试剂具有明显更强的抗增殖活性。为了寻找这一观察结果的机制，我们确定 [C-14]1,25(OH)(2)D-3-3-BE 快速共价标记人重组 1 α,25-二羟基维生素 D-3 受体 (reVDR)（
1 alpha,25-Dihydroxyvitamin D-3-3-bromoacetate (1,25-(OH)(2)D-3-3-BE), an affinity labeling analog of 1 alpha,25-dihydroxyvitamin D-3 (1,25(OH)(2)D-3), displayed stronger antiproliferative activities than 1,25(OH)(2)D-3 at 10(-10)- 10(-6) M dose levels in cultured human keratinocytes (CHK). Additionally, preincubation of the cells with 10(-6) M 1,25(OH)(2)D-3, followed by treatment with various doses of 1,25(OH)(2)D-3-3-BE, resulted in a significantly stronger antiproliferative activity by the mixture than individual reagents at every dose level. To search for a mechanism of this observation, we determined that [C-14]1,25(OH)(2)D-3-3-BE covalently labeled human recombinant 1 alpha,25-dihydroxyvitamin D-3 receptor (reVDR) swiftly (