Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor

Y Zheng, K Balasubramanyam, M Cebrat… - Journal of the …, 2005 - ACS Publications
Y Zheng, K Balasubramanyam, M Cebrat, D Buck, F Guidez, A Zelent, RM Alani, PA Cole
Journal of the American Chemical Society, 2005ACS Publications
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.
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.
ACS Publications