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

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 languageEnglish
Pages (from-to)357-358
Number of pages2
JournalChemical and Pharmaceutical Bulletin
Volume51
Issue number3
Publication statusPublished - 2003 Mar
Externally publishedYes

Fingerprint

Calcitriol Receptors
Vitamin D
Calcitriol
Hydroxyl Radical
Hydrogen bonds
Hormones
2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3

Keywords

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

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Pharmacology

Cite this

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

Kittaka, A, Kurihara, M, Peleg, S, Suhara, Y & Takayama, H 2003, '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', Chemical and Pharmaceutical Bulletin, vol. 51, no. 3, pp. 357-358.
Kittaka A, Kurihara M, Peleg S, Suhara Y, Takayama H. 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. Chemical and Pharmaceutical Bulletin. 2003 Mar;51(3):357-358.
Kittaka, Atsushi ; Kurihara, Masaaki ; Peleg, Sara ; Suhara, Yoshitomo ; Takayama, Hiroaki. / 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. In: Chemical and Pharmaceutical Bulletin. 2003 ; Vol. 51, No. 3. pp. 357-358.
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