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

doi:10.1021/ja0558544

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

Medicine

Research output: Contribution to journal › Article › peer-review

53 Scopus citations

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 language	English (US)
Pages (from-to)	17182-17183
Number of pages	2
Journal	Journal of the American Chemical Society
Volume	127
Issue number	49
DOIs	https://doi.org/10.1021/ja0558544
State	Published - Dec 14 2005

ASJC Scopus subject areas

Catalysis
Chemistry(all)
Biochemistry
Colloid and Surface Chemistry

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10.1021/ja0558544

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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; 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 journal › Article › peer-review

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AU - Cole, Philip A.

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

Abstract

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