Biological activities of 2α-substituted analogues of 1α,25-dihydroxyvitamin D3 in transcriptional regulation and human promyelocytic leukemia (HL-60) cell proliferation and differentiation

Eiji Takahashi, Kimie Nakagawa, Yoshitomo Suhara, Atsushi Kittaka, Ken Ichi Nihei, Katsuhiro Konno, Hiroaki Takayama, Keiichi Ozono, Toshio Okano

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21 Citations (Scopus)


Biological activities of 2α-substituted 1α,25-dihydroxyvitamin D3 analogues were evaluated in vitro. Their binding affinity was examined with calf thymus cytosolic vitamin D receptor (VDR) and rat plasma vitamin D-binding protein (DBP). In addition, the transcriptional activity of the analogues was measured using a rat 25-hydroxyvitamin D3-24- hydroxylase gene promoter, a human osteocalcin gene promoter, and VDR-GAL4 system. This study investigated the biological activities of 2α-substituted analogues in comparison with 2β-substitued analogues at the molecular level, with regard to the structural differences of alkyl, hydroxyalkyl, hydroxyalkoxy substituents at the 2-position of 1α,25-dihydroxyvitamin D3.

Original languageEnglish
Pages (from-to)2246-2250
Number of pages5
JournalBiological and Pharmaceutical Bulletin
Issue number11
Publication statusPublished - 2006 Nov 1



  • 1α,25-dihydroxyvitamin D
  • 2α-substituted analogue
  • Cell cycle arrest
  • Cell differentiation
  • Gene transactivation

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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