title: Discovery and mechanism of natural products as modulators of histone acetylation.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry, University of Florida, Gainesville, 32610, USA.
authors.forename: Lilibeth A
authors.initials: LA
authors.lastname: Salvador
authors.forename: Hendrik
authors.initials: H
authors.lastname: Luesch
mesh_terms: D000107:Acetylation; D001688:Biological Products / Q000737:chemistry / Q000494:pharmacology*; D055808:Drug Discovery; D006657:Histones / Q000378:metabolism*; D011499:Protein Processing, Post-Translational
chemical_list: D001688:Biological Products; D006657:Histones