期刊
STEROIDS
卷 154, 期 -, 页码 -出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.steroids.2019.108536
关键词
Vitamin D; Calcioic acid; Vitamin D receptor; Natural product synthesis
资金
- University of Wisconsin-Milwaukee
- UWM Research Growth Initiative
- National Institutes of Health [R03DA031090]
- UWM Research Foundation
- Lynde and Harry Bradley Foundation
- Richard and Ethel Herzfeld Foundation
- National Science Foundation, Division of Chemistry [CHE-1625735]
- Milwaukee Institute for Drug Discovery
Herein, we describe the synthesis of calcioic acid following a recently developed synthetic strategy for calcitroic acid. Several improvements to reaction conditions were made, which resulted in higher yields. The improved workup and isolation procedures are described. Furthermore, we investigated the interaction between the vitamin D receptor (VDR) and calcioic acid. Calcioic acid was able to bind VDR with a binding constant of 71 mu M, In cells, calcioic acid reduced the transcription of VDR target gene CYP24A1 in the presence 1 alpha,25-dihydroxyvitamin D-3 (1,25(OH)(2)D-3) but did not induce the transcription of CYP24A1. Therefore, calcioic acid is a very weak VDR antagonist. With the generation of gram quantities, further studies are expected to reveal if calcioic acid is solely a water-soluble metabolite of vitamin D or if it mediates other biological functions through bio-molecules other than VDR.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据