301. Vitamin D analogs and coactivators.
- Author
-
Eelen G, Verlinden L, De Clercq P, Vandewalle M, Bouillon R, and Verstuyf A
- Subjects
- Acetyltransferases metabolism, Calcitriol pharmacology, Carrier Proteins metabolism, Histone Acetyltransferases, Humans, Nerve Tissue Proteins metabolism, Nuclear Receptor Coactivator 1, Nuclear Receptor Coactivator 2 metabolism, Nuclear Receptor Coactivator 3, Transcription Factors metabolism, Transcription, Genetic drug effects, p300-CBP Transcription Factors metabolism, Calcitriol analogs & derivatives, Receptors, Calcitriol metabolism, Trans-Activators metabolism
- 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.
- Published
- 2006