Mechanisms for the selective action of Vitamin D analogs
Mechanisms for the selective action of Vitamin D analogs
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DOI：
10.1016/j.jsbmb.2005.06.013
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发表时间：
2005-10-01
影响因子：
4.1
通讯作者：
Verstuyf, A
中科院分区：
文献类型：
--
作者：
Bouillon, R;Verlinden, L;Verstuyf, A
1，25（OH）（2）D-3的非经典效应为免疫调节（例如自身免疫疾病和移植排斥）、抑制细胞增殖（例如牛皮癣、癌症）和诱导细胞分化（例如癌症）创造了可能的治疗应用。与使用1，25（OH）（2）D-3相关的主要缺点是其钙离子效应，这妨碍了药理学浓度的应用。现在有几种类似物在适当的体内模型中进行测试时，显示出对特定效应（例如抗癌或免疫效应或骨抑制与高钙血症）的适度至良好的选择性。这种选择性的分子基础只被部分理解，可能是一个可变的混合机制。(c)2005爱思唯尔有限公司保留所有权利。
The non-classical effects of 1,25(OH)(2)D-3 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)(2)D-3 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. (c) 2005 Elsevier Ltd. All rights reserved.