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Design and biological evaluation of tetrahydro-β-carboline derivatives as highly potent histone deacetylase 6 (HDAC6) inhibitors

Leonhardt, Michel ; Sellmer, Andreas ; Krämer, Oliver H. ; Dove, Stefan ; Elz, Sigurd ; Kraus, Birgit ; Beyer, Mandy ; Mahboobi, Siavosh


Various diseases are related to epigenetic modifications. Histone deacetylases (HDACs) and histone acetyl transferases (HATS) determine the pattern of histone acetylation, and thus are involved in the regulation of gene expression. First generation histone deacetylase inhibitors (HDACi) are unselective, hinder all different kinds of zinc dependent HDACs and additionally cause several side ...


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