Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids |
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| Authors: | Marc Lamblin Basel Dabbas Russell Spingarn Rodrigo Mendoza-Sanchez Tian-Tian Wang Beum-Soo An Dao Chao Huang Richard Kremer John H White James L Gleason |
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| Institution: | 1. Department of Chemistry, McGill University, Montreal, QC, Canada;2. Department of Physiology, McGill University, Montreal, QC, Canada;3. Department of Medicine, McGill University, Montreal, QC, Canada |
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| Abstract: | Incorporation of zinc-binding groups into the side-chain of 1α,25-dihydroxyvitamin D3 (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. |
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