Cinnamoyl compounds as simple molecules that inhibit p300 histone acetyltransferase.
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.
Costi
Roberta
R
Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Università di Roma La Sapienza, P.le A. Moro 5, I-00185 Roma, Italy.
Di Santo
Roberto
R
Artico
Marino
M
Miele
Gaetano
G
Valentini
Paola
P
Novellino
Ettore
E
Cereseto
Anna
A
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
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