Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.

Article Details

Citation

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
DrugTargetPropertyMeasurementpHTemperature (°C)
CalcitriolVitamin D3 receptorIC 50 (nM)13N/AN/ADetails
VorinostatHistone deacetylase 2IC 50 (nM)210N/AN/ADetails
VorinostatHistone deacetylase 3IC 50 (nM)150N/AN/ADetails
VorinostatHistone deacetylase 6IC 50 (nM)350N/AN/ADetails