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

Yujun Zheng, Karanam Balasubramanyam, Marek Cebrat, Donald Buck, Fabien Guidez, Arthur Zelent, Rhoda M. Alani, Philip A. Cole

Research output: Contribution to journalArticle

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.

Original languageEnglish (US)
Pages (from-to)17182-17183
Number of pages2
JournalJournal of the American Chemical Society
Volume127
Issue number49
DOIs
StatePublished - Dec 14 2005

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ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)
  • Biochemistry
  • Colloid and Surface Chemistry

Cite this

Zheng, Y., Balasubramanyam, K., Cebrat, M., Buck, D., Guidez, F., Zelent, A., Alani, R. M., & Cole, P. A. (2005). Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor. Journal of the American Chemical Society, 127(49), 17182-17183. https://doi.org/10.1021/ja0558544