title: Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases.
abstract: Pentadecylidenemalonate 1b, a simplified analogue of anacardic acid, was identified as the first mixed activator/inhibitor of histone acetyltransferases (HATs). It potentiates PCAF HAT activity while inhibiting those of p300/CBP and recombinant CBP. The remarkable apoptotic effect together with the ability to selectively acetylate histone versus non-histone substrates appoint 1b as a lead for the development of anticancer drugs.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy. gsbardella@unisa.it
authors.forename: Gianluca
authors.initials: G
authors.lastname: Sbardella
authors.forename: Sabrina
authors.initials: S
authors.lastname: Castellano
authors.forename: Caterina
authors.initials: C
authors.lastname: Vicidomini
authors.forename: Dante
authors.initials: D
authors.lastname: Rotili
authors.forename: Angela
authors.initials: A
authors.lastname: Nebbioso
authors.forename: Marco
authors.initials: M
authors.lastname: Miceli
authors.forename: Lucia
authors.initials: L
authors.lastname: Altucci
authors.forename: Antonello
authors.initials: A
authors.lastname: Mai
mesh_terms: D000107:Acetylation; D000466:Alkadienes / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects* / Q000502:physiology; D002453:Cell Cycle / Q000187:drug effects* / Q000502:physiology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D051548:Histone Acetyltransferases / Q000037:antagonists & inhibitors*; D006801:Humans; D008314:Malonates / Q000737:chemistry*; D008956:Models, Chemical; D020298:U937 Cells; D050880:p300-CBP Transcription Factors / Q000037:antagonists & inhibitors; D000099224:p300-CBP-Associated Factor
chemical_list: D000466:Alkadienes; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D051548:Histone Acetyltransferases; D008314:Malonates; D050880:p300-CBP Transcription Factors; D000099224:p300-CBP-Associated Factor; C000591545:pentadecylidenemalonate 1b