Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
Article Details
- CitationCopy to clipboard
Lamblin M, Dabbas B, Spingarn R, Mendoza-Sanchez R, Wang TT, An BS, Huang DC, Kremer R, White JH, Gleason JL
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
Bioorg Med Chem. 2010 Jun 1;18(11):4119-37. doi: 10.1016/j.bmc.2010.03.078. Epub 2010 Apr 7.
- PubMed ID
- 20452225 [ View in PubMed]
- Abstract
Incorporation of zinc-binding groups into the side-chain of 1alpha,25-dihydroxyvitamin D(3) (1,25D) fully bifunctional hybrid molecules which act both as vitamin D receptor agonists and histone deacetylase inhibitors. These bifunctional hybrids display in vitro antiproliferative activity against the AT84 squamous carcinoma cell line while lacking the in vivo hypercalcemic effects of 1,25D.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Calcitriol Vitamin D3 receptor IC 50 (nM) 13 N/A N/A Details Vorinostat Histone deacetylase 2 IC 50 (nM) 210 N/A N/A Details Vorinostat Histone deacetylase 3 IC 50 (nM) 150 N/A N/A Details Vorinostat Histone deacetylase 6 IC 50 (nM) 350 N/A N/A Details