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Vitamin D analogs and coactivators

Eelen, G.; Verlinden, L.; De Clercq, P.; Vandewalle, M.; Bouillon, R.; Verstuyf, A.

Anticancer Research 26(4a): 2717-2721

2006

ISSN/ISBN: 0250-7005
PMID: 16886682
Document Number: 597569
The secosteroid hormone 1a,25-dihydroxyvitamin D-3 [1,25-(OH)(2)D-3] has potent antiproliferative and prodifterentiating actions on a wide variety of normal as well as malignant cell types. Strong calcemic effects obstruct the actual application of 1,25-(OH)(2)D-3 for the treatment of hyperproliferative disorders such as cancer. To overcome this problem, structural analogs of 1,25-(OH)(2)D-3 have been designed with a clear dissociation between antiproliferative and calcemic effects. This review focuses on the molecular mode of action of different 1,25-(OH)(2)D-3 analogs and, in particular, on the recruitment of cofactor molecules to the vitamin D receptor by these analogs.

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