摘要
活性维生素D3除了具有调节钙磷代谢的功能外,还是一种细胞循环调节剂,影响细胞的增殖、分化和凋亡。活性维生素D3配体,通过与维生素D受体结合,在体内发挥多种多样的生理学功能,临床上可用来治疗炎症、皮肤病、骨质疏松、癌症和免疫疾病等。为了减少钙血症等不良反应,并使活性维生素D3的各种生理学作用相分离,到目前为止已经合成出3 000余个活性维生素D3衍生物。该文对活性维生素D3的临床应用、构效关系及其研究最新进展进行综述。
The hormonally active vitamin 133, lα, 25-dihydroxyvitamin D3 [ 1, 25-（OH）2D3 ], is now well recognized as an important cell-cycle regulator, which influences cell proliferation, differentiation and apotosis, in addition to possessing a regulatory effects on calcium and phosphorus metabolism, The plethora of actions of 1, 25-（OH）2D3 in various systems suggested wide clinical applications of vitamin D nuclear receptor （VDR） ligands in treatments of inflammation, dermatological indication, osteoporosis, cancers and autoimmune diseases. More than 3 000 vitamin D3 analogues have been synthesized in order to reduce the calcium side effects while maintaining the transactivation potency of these ligands. The clinical roles of 1, 25-（OH）2D3, the structure-activity relationships of the active vitamin D3 analogues, as well as the recent development on the active vitamin D3 researches are briefly introduced in this review.
出处
《中国药物化学杂志》
CAS
CSCD
2006年第5期311-315,共5页
Chinese Journal of Medicinal Chemistry
关键词
药物化学
构效关系
综述
活性维生素D3
维生素D核受体
钙磷代谢
medicinal chemistry
structure-activity relationships
review
1α, 25- dihydroxyvitamin D3
vitamin D nuclear receptor （VDR）
calcium and phosphorus metabolism
