Vitamin D analogs and coactivators.

Guy Eelen, Lieve Verlinden, Pierre De Clercq, Maurits Vandewalle, Roger Bouillon, Annemieke Verstuyf

Journal: Anticancer research 2006;26(4A):2717-21

PMID: 16886682

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Abstract

The secosteroid hormone 1alpha,25-dihydroxyvitamin D3 [1,25-(OH)2D3] has potent antiproliferative and prodifferentiating actions on a wide variety of normal as well as malignant cell types. Strong calcemic effects obstruct the actual application of 1,25-(OH)2D3 for the treatment of hyperproliferative disorders such as cancer. To overcome this problem, structural analogs of 1,25-(OH)2D3 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)2D3 analogs and, in particular, on the recruitment of cofactor molecules to the vitamin D receptor by these analogs.

Address: Laboratorium voor Experimentele Geneeskunde en Endocrinologie, Katholieke Universiteit Leuven, Gasthuisberg, Herestraat 49, B-3000 Leuven, Belgium.

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MeSH Terms: Acetyltransferases, Calcitriol, Carrier Proteins, Histone Acetyltransferases, Humans, Nerve Tissue Proteins, Nuclear Receptor Coactivator 1, Nuclear Receptor Coactivator 2, Nuclear Receptor Coactivator 3, Receptors, Calcitriol, Trans-Activators, Transcription Factors, Transcription, Genetic, p300-CBP Transcription Factors