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

doi:10.1248/bpb.29.2246

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 journal › Article › peer-review

23 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 language	English
Pages (from-to)	2246-2250
Number of pages	5
Journal	Biological and Pharmaceutical Bulletin
Volume	29
Issue number	11
DOIs	https://doi.org/10.1248/bpb.29.2246
Publication status	Published - 2006 Nov
Externally published	Yes

Keywords

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

ASJC Scopus subject areas

Pharmacology
Pharmaceutical Science

Access to Document

10.1248/bpb.29.2246

Cite this

Takahashi, E., Nakagawa, K., Suhara, Y., Kittaka, A., Nihei, K. I., Konno, K., Takayama, H., Ozono, K., & Okano, T. (2006). Biological activities of 2α-substituted analogues of 1α,25-dihydroxyvitamin D₃ in transcriptional regulation and human promyelocytic leukemia (HL-60) cell proliferation and differentiation. Biological and Pharmaceutical Bulletin, 29(11), 2246-2250. https://doi.org/10.1248/bpb.29.2246

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 et al.

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

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

Takahashi, E, Nakagawa, K, Suhara, Y, Kittaka, A, Nihei, KI, Konno, K, Takayama, H, Ozono, K & Okano, T 2006, 'Biological activities of 2α-substituted analogues of 1α,25-dihydroxyvitamin D₃ in transcriptional regulation and human promyelocytic leukemia (HL-60) cell proliferation and differentiation', Biological and Pharmaceutical Bulletin, vol. 29, no. 11, pp. 2246-2250. https://doi.org/10.1248/bpb.29.2246

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