Tokyo University of Agriculture and Technology, Department of Biotechnology and Engineering, Japan.
Tokyo University of Agriculture and Technology, Department of Biotechnology and Engineering, Japan.
J Steroid Biochem Mol Biol. 2018 Mar;177:240-246. doi: 10.1016/j.jsbmb.2017.07.017. Epub 2017 Jul 27.
(23S,25R)-1α,25-Dihydroxyvitamin D 26,23-lactone (calcitriol lactone) is a major metabolite of 1α,25-dihydroxyvitamin D that binds to vitamin D receptor (VDR) and exhibits various biological activities. This lactone and its derivatives are considered to have potential as drug candidates to treat VDR-related diseases, but their biological activities have not yet been fully characterized, mainly because of their limited availability by chemical synthesis. This review deals with synthetic studies of calcitriol lactone, and its derivatives, i.e., methylene lactones (TEI-9647 and its derivatives) and calcitriol lactams (DLAMs). We also discuss their biological activities, VDR-binding affinity and structure-activity relationships.
(23S,25R)-1α,25-二羟维生素 D26,23-内酯（骨化三醇内酯）是 1α,25-二羟维生素 D 的主要代谢产物，与维生素 D 受体（VDR）结合并表现出多种生物学活性。这种内酯及其衍生物被认为是治疗 VDR 相关疾病的潜在药物候选物，但它们的生物学活性尚未得到充分表征，主要是因为它们通过化学合成的有限可用性。这篇综述涉及骨化三醇内酯及其衍生物，即亚甲基内酯（TEI-9647 及其衍生物）和骨化三醇内酰胺（DLAMs）的合成研究。我们还讨论了它们的生物学活性、VDR 结合亲和力和构效关系。
