title: Chemical biology of histone acetyltransferase natural compounds modulators.
abstract: Histone acetyltransferases (HATs) are a class of epigenetic enzymes crucial for chromatin restructuring and transcriptional regulation in eukaryotic cells, thus being a promising target for therapeutic development. Nonetheless, differently from histone deacetylases (HDACs) inhibitors, there is still paucity of small-molecule modulators of HAT activity. After a decline during past decade, natural products and their derivatives could be once again a valuable tool in the lead discovery process and meet such need of Novel Chemical Entities (NCEs). In this review, we will provide a comprehensive summary on the discovery of small-molecule HAT modulators from naturally occurring molecular scaffolds.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Salerno, Via Ponte Don Melillo, 84084, Fisciano (SA), Italy.
authors.forename: Fabrizio Dal
authors.initials: FD
authors.lastname: Piaz
authors.forename: Antonio
authors.initials: A
authors.lastname: Vassallo
authors.forename: Osmany Cuesta
authors.initials: OC
authors.lastname: Rubio
authors.forename: Sabrina
authors.initials: S
authors.lastname: Castellano
authors.forename: Gianluca
authors.initials: G
authors.lastname: Sbardella
authors.forename: Nunziatina
authors.initials: N
authors.lastname: De Tommasi
mesh_terms: D000470:Alkaloids / Q000737:chemistry / Q000378:metabolism; D048729:Anacardic Acids / Q000737:chemistry / Q000378:metabolism; D000818:Animals; D001577:Benzophenones / Q000737:chemistry / Q000378:metabolism; D016227:Benzoquinones / Q000737:chemistry / Q000378:metabolism; D001688:Biological Products / Q000737:chemistry* / Q000378:metabolism*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism*; D005419:Flavonoids / Q000737:chemistry / Q000378:metabolism; D051548:Histone Acetyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D006801:Humans; D010455:Peptides / Q000737:chemistry / Q000378:metabolism; D010636:Phenols / Q000737:chemistry / Q000378:metabolism; D059808:Polyphenols
chemical_list: D000470:Alkaloids; D048729:Anacardic Acids; D001577:Benzophenones; D016227:Benzoquinones; D001688:Biological Products; D004791:Enzyme Inhibitors; D005419:Flavonoids; D010455:Peptides; D010636:Phenols; D059808:Polyphenols; C121576:polyisoprenyl benzophenone; C004532:quinone; D051548:Histone Acetyltransferases