Screening of amide analogues of Trichostatin A in cultures of primary rat hepatocytes: search for potent and safe HDAC inhibitors

Joanna Fraczek, Sarah Deleu, Aneta Lukaszuk, Yordanova Doktorova Tatyana, Dirk Tourwe, Albert Geerts, Tamara Vanhaecke, Karin Vanderkerken, Vera Rogiers

Research output: Contribution to journalArticlepeer-review

9 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)338-346
Number of pages9
JournalInvest New Drugs
Volume27
Publication statusPublished - 2009

Keywords

  • HISTONE DEACETYLASE INHIBITORS
  • HYDROXAMIC ACIDS
  • DIFFERENTIATION
  • APOPTOSIS
  • CANCER
  • primary hepatocytes

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    Jennifer Bolleyn (Speaker)

    27 Feb 2014

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    Karin Vanderkerken (Participant)

    27 Feb 2014

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    Eva De Smedt (Participant)

    27 Feb 2014

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