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

Research output: Contribution to journalArticle

21 Citations (Scopus)

Abstract

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
Volume29
Issue number11
DOIs
Publication statusPublished - 2006 Nov
Externally publishedYes

Keywords

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

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Biological activities of 2α-substituted analogues of 1α,25-dihydroxyvitamin D3 in transcriptional regulation and human promyelocytic leukemia (HL-60) cell proliferation and differentiation. / Takahashi, Eiji; Nakagawa, Kimie; Suhara, Yoshitomo; Kittaka, Atsushi; Nihei, Ken Ichi; Konno, Katsuhiro; Takayama, Hiroaki; Ozono, Keiichi; Okano, Toshio.

In: Biological and Pharmaceutical Bulletin, Vol. 29, No. 11, 11.2006, p. 2246-2250.

Research output: Contribution to journalArticle

Takahashi, Eiji ; Nakagawa, Kimie ; Suhara, Yoshitomo ; Kittaka, Atsushi ; Nihei, Ken Ichi ; Konno, Katsuhiro ; Takayama, Hiroaki ; Ozono, Keiichi ; Okano, Toshio. / Biological activities of 2α-substituted analogues of 1α,25-dihydroxyvitamin D3 in transcriptional regulation and human promyelocytic leukemia (HL-60) cell proliferation and differentiation. In: Biological and Pharmaceutical Bulletin. 2006 ; Vol. 29, No. 11. pp. 2246-2250.
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AU - Nihei, Ken Ichi

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