Effects of alkyl side chains and terminal hydrophilicity on vitamin D receptor (VDR) agonistic activity based on the diphenylpentane skeleton
Effects of alkyl side chains and terminal hydrophilicity on vitamin D receptor (VDR) agonistic activity based on the diphenylpentane skeleton
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基于二苯基戊烷骨架的烷基侧链和末端亲水性对维生素 D 受体 (VDR) 激动活性的影响
DOI：
10.1016/j.bmcl.2015.09.030
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发表时间：
2015
期刊：
影响因子：
--
通讯作者：
Masaaki Kurihara
中科院分区：
文献类型：
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作者：
Takashi Misawa;Momoko Yorioka;Yosuke Demizu;Tomomi Noguchi-Yachide;Nobumichi Ohoka;Megumi Kurashima-Kinoshita;Hitomi Motoyoshi;Hisao Nojiri;Atsushi Kittaka;Makoto Makishima;Mikihiko Naito;Masaaki Kurihara
维生素 D 受体 (VDR) 是核受体 (NR) 的一个家族，可调节免疫系统、钙稳态和细胞增殖等生理效应。我们合成了带有基于二苯基戊烷骨架的长烷基链的非甾体VDR配体。使用报告基因测定和HL-60细胞分化诱导测定评估合成化合物的VDR介导的转录活性。我们在此描述了结构-活性关系以及烷基链长度对 VDR 介导的转录活性的影响。
Vitamin D receptor (VDR) is a family of nuclear receptors (NR) that regulates physiological effects such as the immune system, calcium homeostasis, and cell proliferation. We synthesized non-secosteroidal VDR ligands bearing a long alkyl chain based on the diphenylpentane skeleton. The VDR-mediated transcriptional activities of the synthesized compounds were evaluated using a reporter gene assay and HL-60 cell differentiation-inducing assay. We herein described the structure–activity relationship and effects of alkyl-chain length on VDR-mediated transcriptional activity.