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. © 2008 Springer Science+Business Media, LLC.
CITATION STYLE
Fraczek, J., Deleu, S., Lukaszuk, A., Doktorova, T., Tourwé, D., Geerts, A., … Rogiers, V. (2009). Screening of amide analogues of Trichostatin A in cultures of primary rat hepatocytes: Search for potent and safe HDAC inhibitors. Investigational New Drugs, 27(4), 338–346. https://doi.org/10.1007/s10637-008-9180-x
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