title: Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor.
abstract: 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.
authors.affiliation: Department of Pharmacology, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA.
authors.forename: Yujun
authors.initials: Y
authors.lastname: Zheng
authors.forename: Karanam
authors.initials: K
authors.lastname: Balasubramanyam
authors.forename: Marek
authors.initials: M
authors.lastname: Cebrat
authors.forename: Donald
authors.initials: D
authors.lastname: Buck
authors.forename: Fabien
authors.initials: F
authors.lastname: Guidez
authors.forename: Arthur
authors.initials: A
authors.lastname: Zelent
authors.forename: Rhoda M
authors.initials: RM
authors.lastname: Alani
authors.forename: Philip A
authors.initials: PA
authors.lastname: Cole