Affinity of 22-oxa-1,25(OH)2D3 for 1,25-dihydroxyvitamin D receptor and its effects on the synthesis of osteocalcin in human osteosarcoma cells.
A new 1,25-dihydroxyvitamin D3 analog, 22-oxa-1,25(OH)2D3, which may have pharmaceutical use, e.g., in the treatment of psoriasis, was studied using cultured MG-63 human osteosarcoma cells. We found that the new compound binds to 1,25-dihydroxyvitamin D receptors and regulates receptor mRNA levels like the natural ligand. Our results also indicate that 22-oxa-1,25(OH)2D3 induces the synthesis of osteocalcin and the activity of alkaline phosphatase in MG-63 cells through a receptor-mediated process identically with 1,25(OH)2D3.
Valaja
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Department of Biochemistry and Biotechnology, University of Kuopio, Finland.
Mahonen
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Pirskanen
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Mäenpää
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PH
D000469:Alkaline Phosphatase / Q000378:metabolism; D001667:Binding, Competitive; D001692:Biological Transport; D002117:Calcitriol / Q000031:analogs & derivatives* / Q000378:metabolism* / Q000494:pharmacology; D002460:Cell Line; D006801:Humans; D007700:Kinetics; D015675:Osteocalcin / Q000096:biosynthesis*; D012516:Osteosarcoma; D012334:RNA, Neoplasm / Q000235:genetics / Q000302:isolation & purification; D018167:Receptors, Calcitriol; D011987:Receptors, Steroid / Q000187:drug effects / Q000235:genetics / Q000378:metabolism*; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000378:metabolism*
D012334:RNA, Neoplasm; D018167:Receptors, Calcitriol; D011987:Receptors, Steroid; D015675:Osteocalcin; D000469:Alkaline Phosphatase; D002117:Calcitriol; C051883:maxacalcitol