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 journalArticle

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
DOIs
Publication statusPublished - 2003 Mar

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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