Vrije Universiteit Brussel

 

Publications on Multiple Myeloma

Screening of Amide Analogues of Trichostatin A in Cultures of Primary Rat Hepatocytes: Search for Potent and Safe HDAC Inhibitors
  • Screening of Amide Analogues of Trichostatin A in Cultures of Primary Rat Hepatocytes: Search for Potent and Safe HDAC Inhibitors.

    Fraczek J, Deleu S, Lukaszuk A, Doktorova T, Tourwe D, Geerts A, Vanhaecke T, Vanderkerken K, Rogiers V.

    Invest New Drugs Sep 30 ([Epub ahead of print]), , 2008.

    Abstract:
    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.

 

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