Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids
| Autor: | Russell Spingarn, John H. White, Dao Chao Huang, Beum-Soo An, Basel Dabbas, James L. Gleason, Richard Kremer, Rodrigo Mendoza-Sanchez, Marc Lamblin, Tian-Tian Wang |
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| Rok vydání: | 2010 |
| Předmět: |
Agonist
medicine.drug_class Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Biochemistry Calcitriol receptor Cell Line Tumor Drug Discovery medicine Humans Vitamin D Receptor Molecular Biology Cell Proliferation biology Chemistry Organic Chemistry Histone deacetylase inhibitor Squamous carcinoma Histone Deacetylase Inhibitors Zinc Nuclear receptor Enzyme inhibitor Carcinoma Squamous Cell biology.protein Receptors Calcitriol Molecular Medicine Histone deacetylase |
| Zdroj: | Bioorganic & Medicinal Chemistry. 18:4119-4137 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2010.03.078 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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