Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor.
Fiche publication
Date publication
décembre 2005
Journal
Journal of the American Chemical Society
Auteurs
Membres identifiés du Cancéropôle Est :
Dr GUIDEZ Fabien
Tous les auteurs :
Zheng Y, Balasubramanyam K, Cebrat M, Buck D, Guidez F, Zelent A, Alani RM, Cole PA
Lien Pubmed
Résumé
This paper describes the first potent and selective p300 histone acetyltransferase (HAT) inhibitor which is effective in live cells. This compound 7 is a coenzyme A analogue conjugated to a cell permeabilizing oligoArg peptide via disulfide linkage. This compound was shown to block cellular histone acetylation and transcription using a p300-sensitive reporter. It should thus be broadly useful for dissecting the role of p300 HAT activity in physiologic and disease states.
Référence
J Am Chem Soc. 2005 12 14;127(49):17182-3