The first locked side-chain analogues of calcitriol (1α,25-dihydroxyvitamin D3) induce vitamin D receptor transcriptional activity

被引：26
|
作者：
Pérez-García, X
Rumbo, A
Larriba, MJ
Ordóñez, P
Muñoz, A
Mouriño, A
机构：
[1] Univ Santiago de Compostela, CSIC, Dept Quim Organ & Unidad Asociada, Santiago De Compostela 15706, Spain
[2] UAM, CSIC, Inst Invest Biomed, Madrid 28029, Spain
来源：
ORGANIC LETTERS | 2003年 / 5卷 / 22期
关键词：
D O I：
10.1021/ol0351246
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
[GRAPHIC] We describe the synthesis of the first locked side-chain analogues of the natural hormone 1alpha,25-(OH)(2)-D-3 and their effects on gene transcription in human colon cancer cells. Analogue 2 was more potent than 1alpha,25-(OH)(2)-D-3 at inducing vitamin D receptor (VDR) transcriptional activity. Analogues 3a and 3b show potency similar to that of 1alpha,25-(OH)(2)-D-3, whereas 3c was less active. The novel analogues efficiently bind VDR in vivo to induce transcription from a consensus vitamin D responsive element (VDRE).
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页码：4033 / 4036
页数：4
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