Discovery and mechanism of natural products as modulators of histone acetylation.

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 biological effects.