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.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Acetyltransferases / metabolism
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Calcitriol / analogs & derivatives*
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Calcitriol / pharmacology
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Carrier Proteins / metabolism
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Histone Acetyltransferases
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Humans
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Nerve Tissue Proteins / metabolism
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Nuclear Receptor Coactivator 1
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Nuclear Receptor Coactivator 2 / metabolism
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Nuclear Receptor Coactivator 3
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Receptors, Calcitriol / metabolism*
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Trans-Activators / metabolism*
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Transcription Factors / metabolism
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Transcription, Genetic / drug effects
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p300-CBP Transcription Factors / metabolism
Substances
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Carrier Proteins
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GRIP1 protein, human
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NCOA2 protein, human
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Nerve Tissue Proteins
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Nuclear Receptor Coactivator 2
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Receptors, Calcitriol
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Trans-Activators
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Transcription Factors
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Acetyltransferases
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Histone Acetyltransferases
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NCOA1 protein, human
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NCOA3 protein, human
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Nuclear Receptor Coactivator 1
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Nuclear Receptor Coactivator 3
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p300-CBP Transcription Factors
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Calcitriol