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• W2020389231 abstract "1,25-dihydroxyvitamin D 3 (1,25D) regulates gene expression by signaling through the nuclear vitamin D receptor (VDR) transcription factor and exhibits calcium homeostatic, anticancer, and immunomodulatory properties. Histone deacetylase inhibitors (HDACis) alter nuclear and cytoplasmic protein acetylation, modify gene expression, and have potential for treatment of cancer and other indications. The function of nuclear receptor ligands, including 1,25D, can be enhanced in combination with HDACi. We designed triciferol, a hybrid molecule in which the 1,25D side chain was replaced with the dienyl hydroxamic acid of HDACi trichostatin A. Triciferol binds directly to the VDR, and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Moreover, unlike 1,25D, triciferol induces marked tubulin hyperacetylation, and augments histone acetylation at concentrations that largely overlap those where VDR agonism is observed. Triciferol also exhibits more efficacious antiproliferative and cytotoxic activities than 1,25D in four cancer cell models in vitro . The bifunctionality of triciferol is notable because ( i ) the HDACi activity is generated by modifying the 1,25D side chain without resorting to linker technology and ( ii ) 1,25D and HDACi have sympathetic, but very distinct biochemical targets; the hydrophobic VDR ligand binding domain and the active sites of HDACs, which are zinc metalloenzymes. These studies demonstrate the feasibility of combining HDAC inhibition with nuclear receptor agonism to enhance their therapeutic potential." @default.
• W2020389231 created "2016-06-24" @default.
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• W2020389231 date "2008-06-17" @default.
• W2020389231 modified "2023-09-24" @default.
• W2020389231 title "Incorporation of histone deacetylase inhibition into the structure of a nuclear receptor agonist" @default.
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• W2020389231 doi "https://doi.org/10.1073/pnas.0709279105" @default.
• W2020389231 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2426965" @default.
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