Therapeutic potential of the 2-alkyl and 2-alkylidene-19-nor-(20S)-modified analogs of 1α,25-dihydroxyvitamin D3

被引：11

作者：

DeLuca, HF ^{[1
]}

机构：

[1] Univ Wisconsin, Dept Biochem, Madison, WI 53706 USA

来源：

JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY | 2004年 / 89-90卷 / 1-5期

关键词：

vitamin D and bone; vitamin D analog; bone synthesis; non-calcemic vitamin D analog; parathyroid suppression;

D O I：

10.1016/j.jsbmb.2004.03.104

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

Five analogs of 19-nor-1alpha,25-dihydroxyvitamin D-3 are described that show highly selective and potent activities. The 2-methylene-19-nor(20S)- 1alpha,25-dihydroxyvitamin D-3 (2MD) and its 2alpha-methyl sister are selectively active on the osteoblast. 2MD is bone anabolic and causes bone formation in vivo and in vitro and is being developed as a therapy for bone loss diseases such as osteoporosis. 2-Methylene-19-nor (20S)-bishomo-1alpha-hydroxypregnacalciferol (2BMP) has no activity on calcium in vivo while totally suppressing circulating parathyroid hormone. Its homologs, i.e. 2-methylene-19-nor-1alpha-hydroxy-homopregnacalciferol (2MP) and 2-methylene-19-nor-1alpha-hydroxypregnacalciferol (2MPC) act similarly but are either less selective (2MP) or not as potent (2MPC). These abbreviated side chain analogs will be developed for diseases where a rise in serum calcium is not desired, as for example, cancer, renal osteodystrophy, psoriasis and autoimmune diseases. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：67 / 73

页数：7

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