title: Biological activities of 2alpha-substituted analogues of 1alpha,25-dihydroxyvitamin D3 in transcriptional regulation and human promyelocytic leukemia (HL-60) cell proliferation and differentiation.
abstract: Biological activities of 2alpha-substituted 1alpha,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 2alpha-substituted analogues in comparison with 2beta-substitued analogues at the molecular level, with regard to the structural differences of alkyl, hydroxyalkyl, hydroxyalkoxy substituents at the 2-position of 1alpha,25-dihydroxyvitamin D3.
authors.affiliation: Department of Hygienic Sciences, Kobe Pharmaceutical University, Japan.
authors.forename: Eiji
authors.initials: E
authors.lastname: Takahashi
authors.forename: Kimie
authors.initials: K
authors.lastname: Nakagawa
authors.forename: Yoshitomo
authors.initials: Y
authors.lastname: Suhara
authors.forename: Atsushi
authors.initials: A
authors.lastname: Kittaka
authors.forename: Ken-ichi
authors.initials: K
authors.lastname: Nihei
authors.forename: Katsuhiro
authors.initials: K
authors.lastname: Konno
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Takayama
authors.forename: Keiichi
authors.initials: K
authors.lastname: Ozono
authors.forename: Toshio
authors.initials: T
authors.lastname: Okano
mesh_terms: D000818:Animals; D039481:CD11b Antigen / Q000096:biosynthesis; D002117:Calcitriol / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology*; D002417:Cattle; D002453:Cell Cycle / Q000187:drug effects; D002454:Cell Differentiation / Q000187:drug effects*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D005434:Flow Cytometry; D018922:HL-60 Cells; D006801:Humans; D018950:Lipopolysaccharide Receptors / Q000096:biosynthesis; D008156:Luciferases / Q000235:genetics / Q000378:metabolism; D015394:Molecular Structure; D015675:Osteocalcin / Q000494:pharmacology; D011485:Protein Binding / Q000187:drug effects; D051381:Rats; D018167:Receptors, Calcitriol / Q000235:genetics / Q000378:metabolism; D013250:Steroid Hydroxylases / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D015533:Transcriptional Activation / Q000187:drug effects* / Q000235:genetics; D014162:Transfection; D014809:Vitamin D-Binding Protein / Q000235:genetics / Q000378:metabolism; D065668:Vitamin D3 24-Hydroxylase
chemical_list: D039481:CD11b Antigen; D018950:Lipopolysaccharide Receptors; D018167:Receptors, Calcitriol; D014809:Vitamin D-Binding Protein; D015675:Osteocalcin; D008156:Luciferases; D013250:Steroid Hydroxylases; D065668:Vitamin D3 24-Hydroxylase; D002117:Calcitriol