Histone deacetylase inhibitors that target tubulin
2009; Elsevier BV; Volume: 280; Issue: 2 Linguagem: Inglês
10.1016/j.canlet.2009.01.040
ISSN1872-7980
AutoresJörg Schemies, Wolfgang Sippl, Manfred Jung,
Tópico(s)Ubiquitin and proteasome pathways
ResumoEpigenetics 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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