Design, synthesis and X-ray crystallographic study of new nonsecosteroidal vitamin D receptor ligands

…, S Kakuda, M Takimoto-Kamimura, M Kurihara

Index: Demizu, Yosuke; Takahashi, Takeo; Kaneko, Fumiya; Sato, Yukiko; Okuda, Haruhiro; Ochiai, Eiji; Horie, Kyohei; Takagi, Ken-Ichiro; Kakuda, Shinji; Takimoto-Kamimura, Midori; Kurihara, Masaaki Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 20 p. 6104 - 6107

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Citation Number: 15

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- ...