Evaluation of a photolabile derivative of 1,25-dihydroxyvitamin D3 as a photoaffinity probe for 1,25-dihydroxyvitamin-D3 receptor in chick intestinal cytosol.
Evaluation of a photolabile derivative of 1,25-dihydroxyvitamin D3 as a photoaffinity probe for 1,25-dihydroxyvitamin-D3 receptor in chick intestinal cytosol.
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评估 1,25-二羟基维生素 D3 的光不稳定衍生物作为鸡肠细胞质中 1,25-二羟基维生素-D3 受体的光亲和探针。
DOI：
10.1016/0006-291x(85)91007-1
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发表时间：
1985
影响因子：
3.1
通讯作者：
Holick,MF
中科院分区：
文献类型：
--
作者：
Ray,R;Rose,S;Holick,SA;Holick,MF
本文研究了1α，25-二羟基维生素D_3 -3β-[N-（4-叠氮基-2-硝基苯基）甘氨酸]（1，25-（OH）_2-D_3-ANG）作为1，25-（OH）_2-D_3受体的光亲和探针在鸡小肠胞液中的活性。竞争性结合试验表明，鸡小肠胞浆1，25-（OH）2-D3受体与1，25-（OH）2-D3-ANG的结合效率比与1，25-（OH）2-D3的结合效率低约20倍。在鸡小肠胞浆制剂存在下照射1，25-（OH）2-D3- ANG显著减少随后与3 H-1，25-（OH）2-D3的结合，表明光亲和类似物共价连接到受体上。因此，1，25-（OH）2-D3的硝基芳基叠氮衍生物可能是一种有价值的光亲和探针，用于表征1，25-（OH）2-D3受体。
We evaluated the viability of 1α,25-dihydroxyvitaminD3-3β-[N-(4-azido-2-nitrophenyl)glycinate] (1,25-(OH)2-D3-ANG), an analog of 1α,25-dihydroxyvitamin D3(1,25-(OH)2-D3) as a photoaffinity probe for 1,25-(OH)2-D3receptor in chick intestinal cytosol. A competitive-binding assay revealed that chick intestinal cytosolic 1,25-(OH)2- D3receptor bound to 1,25-(OH)2-D3-ANG approximately 20-times less effectively than it did to 1,25-(OH)2-D3. Irradiation of 1,25-(OH)2-D3- ANG in the presence of chick intestinal cytosolic preparation significantly diminished subsequent binding to3H-1,25-(OH)2-D3, suggesting that the photoaffinity analog was covalently attached to the receptor. Therefore the nitroarylazide derivative of 1,25-(OH)2-D3may be a valuable photoaffinity probe for the characterization of the 1,25-(OH)2-D3receptor.