Screening of amide analogues of Trichostatin A in cultures of primary rat hepatocytes: search for potent and safe HDAC inhibitors
| Autor: | Albert Geerts, Tamara Vanhaecke, Aneta Lukaszuk, Dirk Tourwé, Tatyana Y. Doktorova, Vera Rogiers, Sarah Deleu, Joanna Fraczek, Karin Vanderkerken |
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| Přispěvatelé: | Hematology, Cell Biology and Histology, Chemistry, Organic Chemistry, Toxicology, Dermato-cosmetology and Pharmacognosy, Liver Cell Biology |
| Jazyk: | angličtina |
| Rok vydání: | 2009 |
| Předmět: |
Male
Cell Drug Evaluation Preclinical Histone Deacetylase 1 Pharmacology Biology histone deacetylase inhibitors Rats Sprague-Dawley medicine Cytotoxic T cell Animals Pharmacology (medical) Enzyme Inhibitors HYDROXAMIC ACIDS primary hepatocytes Cells Cultured Cancer apoptosis Biological activity differentiation Amides HDAC1 Rats Trichostatin A medicine.anatomical_structure Oncology Drug development Apoptosis Toxicity Hepatocytes medicine.drug |
| Zdroj: | Vrije Universiteit Brussel |
| Popis: | The vast majority of preclinical studies of HDAC inhibitors (HDAC-I) focus on the drug-target (cancer) cell interaction, whereas little attention is paid to the effects on non-target healthy cells, which could provide decisive information to eliminate potential cytotoxic compounds at a very early stage during drug development. In the current study we used cultures of primary rat hepatocytes as a read out system to select for the most potent HDAC-I in the group of structural analogues of an archetypal HDAC-I, namely Trichostatin A. This kind of approach allowed selecting compounds with high biological activity and with no apparent toxicity towards cultured hepatocytes. |
| Databáze: | OpenAIRE |
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