title: [Current Topics on Vitamin D. Protein interaction and biological action of active vitamin D compounds].
abstract: To express its biological action, active vitamin D3 (1α,25-dihydroxyvitamin D3) interacts with three proteins : vitamin D binding protein (DBP), vitamin D receptor (VDR), and CYP24A1. This article explains how eldecalcitol interacts with these three proteins to achieve its mode of action. The main feature of eldecalcitol's molecular structure is the 3-hydroxypropyloxy group (3-HP group) at the 2β-position. When interacting with DBP, eldecalcitol tightly binds to DBP via the 3-HP group and enhances systemic stability of eldecalcitol. By binding to VDR, the 3-HP group stabilizes the eldecalcitol-VDR complex, which leads to high efficacy. The 3-HP group also interferes with the binding to CYP24A1, which induces residence to CYP24A1 and liver metabolism. These protein interactions constitute the mode of action of eldecalcitol.
authors.affiliation: Research Division, Chugai Pharmaceutical Co., Ltd., Japan.
authors.forename: Yoshiyuki
authors.initials: Y
authors.lastname: Ono
mesh_terms: D000818:Animals; D006801:Humans; D008099:Liver / Q000187:drug effects* / Q000378:metabolism; D010024:Osteoporosis / Q000378:metabolism*; D018167:Receptors, Calcitriol / Q000187:drug effects* / Q000378:metabolism; D014807:Vitamin D / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D014809:Vitamin D-Binding Protein / Q000378:metabolism*; D065668:Vitamin D3 24-Hydroxylase / Q000494:pharmacology*
chemical_list: D018167:Receptors, Calcitriol; D014809:Vitamin D-Binding Protein; C118756:dihydroxy-vitamin D3; D014807:Vitamin D; D065668:Vitamin D3 24-Hydroxylase