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