Tipping the Balance Between Life and Death: Targeting Histone Acetylation for Cancer Therapy

Stephen   A.   Watt; Andrew   P.   South

doi:10.2174/2210303111303020007

Abstract

Epigenetic modifications, such as DNA methylation and histone acetylation, are well established as important players in tumourigenesis and thereby sought after targets in therapeutic intervention. Recent years have seen an increase in the research and clinical development of histone deacetylase (HDAC) inhibitors as anti-cancer agents, but emerging evidence now suggests that the class of enzymes performing the reciprocal function of histone acetylation, histone acetyltransferases (HATs), may also have pivotal roles in cancer progression. Here we discuss the role of HAT complexes in tumourigenesis and their potential as bona fide druggable cancer targets, focusing in particular on the evolutionary conserved TIP60 complex.

Keywords: Acetylation, cancer, epigenetics, HAT inhibitors, histone acetyltransferases, MRGBP, TIP60, tumour therapy.