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Issue 14, 2018
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Effects of 2-substitution on 14-epi-19-nortachysterol-mediated biological events: based on synthesis and X-ray co-crystallographic analysis with the human vitamin D receptor

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Abstract

Both 2α- and 2β-hydroxypropyl substituted 14-epi-1α,25-dihydroxy-19-nortachysterols were synthesized to study the human vitamin D receptor (hVDR) binding affinity, binding configurations, and interactions with amino acid residues in the ligand binding domain of hVDR by X-ray co-crystallographic analysis. In conjunction with our previous results on 14-epi-19-nortachysterol, 2-methylidene-, 2α-methyl-, 2β-methyl, and 2α-hydroxypropoxy-14-epi-19-nortachysterol, we propose a variety of effects of substitution at the C2 position in the 14-epi-19-nortachysterol skeleton on biological activities.

Graphical abstract: Effects of 2-substitution on 14-epi-19-nortachysterol-mediated biological events: based on synthesis and X-ray co-crystallographic analysis with the human vitamin D receptor

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Publication details

The article was received on 19 Jan 2018, accepted on 08 Mar 2018 and first published on 09 Mar 2018


Article type: Paper
DOI: 10.1039/C8OB00158H
Citation: Org. Biomol. Chem., 2018,16, 2448-2455
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    Effects of 2-substitution on 14-epi-19-nortachysterol-mediated biological events: based on synthesis and X-ray co-crystallographic analysis with the human vitamin D receptor

    D. Sawada, S. Kakuda, A. Takeuchi, F. Kawagoe, M. Takimoto-Kamimura and A. Kittaka, Org. Biomol. Chem., 2018, 16, 2448
    DOI: 10.1039/C8OB00158H

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