Kagechika Hiroyuki, Fujii Shinya, Tanatani Aya
Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Japan.
Institute of Molecular and Cellular Biosciences, The University of Tokyo, Japan.
Clin Calcium. 2017;27(11):1579-1586.
Vitamin D plays important roles in many physiological processes, including calcium and phosphate homeostasis, bone metabolism, and immune regulation. An active form of vitamin D, 1α,25(OH)D, binds to vitamin D nuclear receptor(VDR, vitamin D receptor), and regulates expression of specific target genes. Thousands of vitamin D analogs have been synthesized, and the structure-activity relationships of secosteroidal compounds have been examined in detail. On the other hand, development of non-secosteroidal VDR ligands remains limited, and only a few non-secosteroidal VDR ligands with potent activity have been reported so far. Development of novel structures with unique biological profiles would enable the new clinical application of vitamin D function.
维生素D在许多生理过程中发挥着重要作用，包括钙和磷的稳态、骨代谢以及免疫调节。维生素D的活性形式1α,25(OH)D与维生素D核受体（VDR，维生素D受体）结合，并调节特定靶基因的表达。已经合成了数千种维生素D类似物，并且对甾体化合物的构效关系进行了详细研究。另一方面，非甾体类VDR配体的开发仍然有限，迄今为止仅报道了少数具有强效活性的非甾体类VDR配体。开发具有独特生物学特性的新结构将使维生素D功能有新的临床应用。
