Small molecules that modulate histone acetylation by targeting key enzymes mediating this posttranslational
modification – histone acetyltransferases and histone deacetylases – are validated chemotherapeutic agents for the treatment
of cancer. This area of research has seen a rapid increase in interest in the past decade, with the structurally diverse
natural products-derived compounds at its forefront. These secondary metabolites from various biological sources target
this epigenetic modification through distinct mechanisms of enzyme regulation by utilizing a diverse array of pharmacophores.
We review the discovery of these compounds and discuss their modes of inhibition together with their downstream
Keywords: Histone acetylation, histone deacetylases, histone acetyltransferases, natural products, secondary metabolites, Natural Products, chemotherapeutic agents, epigenetic modification, enzyme regulation, DNA
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