2 α-(3-hydroxypropyl)- and 2 α-(3-hydroxypropoxy)-1 α,25-dihydroxyvitamin D3 accessible to vitamin D receptor mutant related to hereditary vitamin D-resistant rickets

Atsushi Kittaka; Masaaki Kurihara; Sara Peleg; Yoshitomo Suhara; Hiroaki Takayama

doi:10.1248/cpb.51.357

2 α-(3-hydroxypropyl)- and 2 α-(3-hydroxypropoxy)-1 α,25-dihydroxyvitamin D₃ accessible to vitamin D receptor mutant related to hereditary vitamin D-resistant rickets

Atsushi Kittaka, Masaaki Kurihara, Sara Peleg, Yoshitomo Suhara, Hiroaki Takayama

Research output: Contribution to journal › Article › peer-review

28 Citations (Scopus)

Abstract

Hereditary vitamin D-resistant rickets (HVDRR) is a genetic disorder caused by mutations in the vitamin D receptor, which lead to resistance to 1 α,25-dihydroxyvitamin D₃ [1 α,25(OH)₂D ₃]. We found that the A ring-modified analogues, 2 α-(3-hydroxypropyl)-and 2 α-(3-hydroxypropoxy)-1 α,25(OH) ₂D₃, (O1C3 and O2C3) can bind better than the natural hormone to the mutant VDR (R274A), which similar to the HVDRR mutant, R274L, had lost the hydrogen bond to the 1 α-hydroxyl group of 1 α,25(OH) ₂D₃.

Original language	English
Pages (from-to)	357-358
Number of pages	2
Journal	Chemical and Pharmaceutical Bulletin
Volume	51
Issue number	3
DOIs	https://doi.org/10.1248/cpb.51.357
Publication status	Published - 2003 Mar
Externally published	Yes

Keywords

2 α-substituted 1 α,25-dihydroxyvitamin D
Docking study
Mutant vitamin D receptor
Potent ligand
Rickets

ASJC Scopus subject areas

Chemistry(all)
Drug Discovery

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2 α-(3-hydroxypropyl)- and 2 α-(3-hydroxypropoxy)-1 α,25-dihydroxyvitamin D₃ accessible to vitamin D receptor mutant related to hereditary vitamin D-resistant rickets. / Kittaka, Atsushi; Kurihara, Masaaki; Peleg, Sara; Suhara, Yoshitomo; Takayama, Hiroaki.

In: Chemical and Pharmaceutical Bulletin, Vol. 51, No. 3, 03.2003, p. 357-358.

Research output: Contribution to journal › Article › peer-review

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abstract = "Hereditary vitamin D-resistant rickets (HVDRR) is a genetic disorder caused by mutations in the vitamin D receptor, which lead to resistance to 1 α,25-dihydroxyvitamin D3 [1 α,25(OH)2D 3]. We found that the A ring-modified analogues, 2 α-(3-hydroxypropyl)-and 2 α-(3-hydroxypropoxy)-1 α,25(OH) 2D3, (O1C3 and O2C3) can bind better than the natural hormone to the mutant VDR (R274A), which similar to the HVDRR mutant, R274L, had lost the hydrogen bond to the 1 α-hydroxyl group of 1 α,25(OH) 2D3.",

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AU - Takayama, Hiroaki

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