| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370656 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
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 D3 and 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.
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Authors
Yosuke Demizu, Takeo Takahashi, Fumiya Kaneko, Yukiko Sato, Haruhiro Okuda, Eiji Ochiai, Kyohei Horie, Ken-ichiro Takagi, Shinji Kakuda, Midori Takimoto-Kamimura, Masaaki Kurihara,