Design, synthesis and X-ray crystallographic study of new nonsecosteroidal vitamin D receptor ligands.
Design, synthesis and X-ray crystallographic study of new nonsecosteroidal vitamin D receptor ligands.
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新型非甾体维生素 D 受体配体的设计、合成和 X 射线晶体学研究。
DOI：
10.1016/j.bmcl.2011.08.047
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发表时间：
2011
影响因子：
2.7
通讯作者：
M. Kurihara
中科院分区：
文献类型：
--
作者：
Yosuke Demizu;Takeo Takahashi;Fumiya Kaneko;Yukiko Sato;H. Okuda;E. Ochiai;Kyohei Horie;Ken;S. Kakuda;M. Takimoto;M. Kurihara
我们设计并合成了与VDR配体结合域的六个氨基酸残基（Tyr143、Ser233、Arg270、Ser274、His301和His393）形成h键的非甾体维生素D受体（VDR）配体。配体YR335表现出与1α，25-二羟基维生素d3和YR301相当的转录活性。对YR335与VDR配体结合域形成的配合物的晶体结构进行了解析，发现YR335与上述6个氨基酸残基形成了氢键。
We designed and synthesized nonsecosteroidal vitamin D receptor (VDR) ligands that formed H-bonds with six amino acid residues (Tyr143, Ser233, Arg270, Ser274, His301 and His393) of the VDR ligand-binding domain. The ligand YR335 exhibited potent transcriptional activity, which was comparable to those of 1α,25-dihydroxyvitamin D3and YR301. The crystal structure of the complex formed between YR335 and the VDR ligand-binding domain was solved, which revealed that YR335 formed H-bonds with the six amino acid residues mentioned above.
影响因子：
15
作者：
S. Swann;J. Bergh;M. Farach-Carson;Cory A. Ocasio;J. Koh
通讯作者：
S. Swann;J. Bergh;M. Farach-Carson;Cory A. Ocasio;J. Koh