Biological Activities of 2α-Substituted Analogues of 1α,25-Dihydroxyvitamin D3 in Transcriptional Regulation and Human Promyelocytic Leukemia (HL-60) Cell Proliferation and Differentiation

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  • Biological Activities of 2.ALPHA.-Substituted Analogues of 1.ALPHA.,25-Dihydroxyvitamin D3 in Transcriptional Regulation and Human Promyelocytic Leukemia (HL-60) Cell Proliferation and Differentiation
  • Biological Activities of 2 アルファ Substituted Analogues of 1 アルファ 25 Dihydroxyvitamin D3 in Transcriptional Regulation and Human Promyelocytic Leukemia HL 60 Cell Proliferation and Differentiation

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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.

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