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 Z Zelent, Rhoda M. Alani, Philip A. Cole

Research output: Contribution to journalArticle

48 Citations (Scopus)

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
Externally publishedYes

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Coenzymes
Histone Acetyltransferases
Acetylation
Transcription
Peptides
Coenzyme A
Disulfides
Histones
p300-CBP-associated factor

ASJC Scopus subject areas

  • Chemistry(all)

Cite this

Zheng, Y., Balasubramanyam, K., Cebrat, M., Buck, D., Guidez, F., Zelent, A. Z., ... 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

Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor. / Zheng, Yujun; Balasubramanyam, Karanam; Cebrat, Marek; Buck, Donald; Guidez, Fabien; Zelent, Arthur Z; Alani, Rhoda M.; Cole, Philip A.

In: Journal of the American Chemical Society, Vol. 127, No. 49, 14.12.2005, p. 17182-17183.

Research output: Contribution to journalArticle

Zheng, Y, Balasubramanyam, K, Cebrat, M, Buck, D, Guidez, F, Zelent, AZ, Alani, RM & Cole, PA 2005, 'Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor', Journal of the American Chemical Society, vol. 127, no. 49, pp. 17182-17183. https://doi.org/10.1021/ja0558544
Zheng, Yujun ; Balasubramanyam, Karanam ; Cebrat, Marek ; Buck, Donald ; Guidez, Fabien ; Zelent, Arthur Z ; Alani, Rhoda M. ; Cole, Philip A. / Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor. In: Journal of the American Chemical Society. 2005 ; Vol. 127, No. 49. pp. 17182-17183.
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