Mechanisms for the selective action of Vitamin D analogs

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• 作者：Roger Bouillon ; Lieve Verlinden ; Guy Eelen ; Pierre De Clercq ; Maurits Vandewalle ; Chantal Mathieu and Annemieke Verstuyf
• 关键词：Vitamin D ; Analogs ; Tissue-selective activity
• 刊名：The Journal of Steroid Biochemistry and Molecular Biology
• 出版年：2005
• 出版时间：2005
• 年：2005
• 卷：97
• 期：1-2
• 页码：21-30
• 全文大小：251 K

文摘

The non-classical effects of 1,25(OH)₂D₃ create possible therapeutic applications for immune modulation (e.g. auto-immune diseases and graft rejection), inhibition of cell proliferation (e.g. psoriasis, cancer) and induction of cell differentiation (e.g. cancer). The major drawback related to the use of 1,25(OH)₂D₃ is its calcemic effect, which prevents the application of pharmacological concentrations. Several analogs are now available that show modest to good selectivity with regard to specific effects (e.g. anticancer or immune effects or bone anabolism versus hypercalcemia) when tested in appropriate in vivo models. The molecular basis for this selectivity is only partially understood and probably a variable mixture of mechanisms.