title: Cinnamoyl compounds as simple molecules that inhibit p300 histone acetyltransferase.
abstract: Cinnamoly compounds 1a-c and 2a-d were designed, synthesized, and in vitro tested as p300 inhibitors. At different degrees, all tested compounds were proven to inactivate p300, particularly, derivative 2c was the most active inhibitor, also showing high specificity for p300 as compared to other histone acetyltransferases. Most notably, 2c showed anti-acetylase activity in mammalian cells. These compounds represent a new class of synthetic inhibitors of p300, characterized by simple chemical structures.
authors.affiliation: Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Università di Roma La Sapienza, P.le A. Moro 5, I-00185 Roma, Italy.
authors.forename: Roberta
authors.initials: R
authors.lastname: Costi
authors.forename: Roberto
authors.initials: R
authors.lastname: Di Santo
authors.forename: Marino
authors.initials: M
authors.lastname: Artico
authors.forename: Gaetano
authors.initials: G
authors.lastname: Miele
authors.forename: Paola
authors.initials: P
authors.lastname: Valentini
authors.forename: Ettore
authors.initials: E
authors.lastname: Novellino
authors.forename: Anna
authors.initials: A
authors.lastname: Cereseto
mesh_terms: D000107:Acetylation; D001597:Benzylidene Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D018797:Cell Cycle Proteins / Q000037:antagonists & inhibitors*; D002463:Cell Membrane Permeability; D002934:Cinnamates / Q000138:chemical synthesis* / Q000494:pharmacology; D003474:Curcumin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology; D003512:Cyclohexanones / Q000138:chemical synthesis* / Q000494:pharmacology; D006367:HeLa Cells; D051548:Histone Acetyltransferases / Q000037:antagonists & inhibitors*; D006657:Histones / Q000378:metabolism; D006801:Humans; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D014157:Transcription Factors / Q000037:antagonists & inhibitors*; D050880:p300-CBP Transcription Factors; D000099224:p300-CBP-Associated Factor
chemical_list: D001597:Benzylidene Compounds; D018797:Cell Cycle Proteins; D002934:Cinnamates; D003474:Curcumin; D003512:Cyclohexanones; D051548:Histone Acetyltransferases; D006657:Histones; D011994:Recombinant Proteins; D014157:Transcription Factors; D050880:p300-CBP Transcription Factors; D000099224:p300-CBP-Associated Factor; C520348:2,6-bis(3-bromo-4-hydroxybenzylidene)cyclohexanone