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  • Title: Histone deacetylase inhibitors that target tubulin.
    Author: Schemies J, Sippl W, Jung M.
    Journal: Cancer Lett; 2009 Aug 08; 280(2):222-32. PubMed ID: 19268440.
    Abstract:
    Epigenetics is defined as heritable changes in gene expression that occur without changes in DNA sequence. Major mechanisms of epigenetics are post-translational histone modifications such as reversible acetylation. Histone deacetylases (HDACs) maintain the acetylation level of histones but also act on non-histone substrates that are involved in signal transduction or cellular transport processes. One important non-histone substrate is tubulin. The isotypes responsible for tubulin deacetylation are HDAC6 and the NAD(+)-dependent histone deacetylase (sirtuin) Sirt2. Here we review the action of those enzymes on tubulin and present an overview over existing inhibitors with a focus on their structural interaction with the targets.
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