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

51 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

Access to Document

10.1021/ja0558544

Fingerprint Dive into the research topics of 'Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor'. Together they form a unique fingerprint.

Cite this

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

@article{730e3c9b30a242818f7ef33e956ee802,

title = "Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor",

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.",

author = "Yujun Zheng and Karanam Balasubramanyam and Marek Cebrat and Donald Buck and Fabien Guidez and Arthur Zelent and Alani, {Rhoda M.} and Cole, {Philip A.}",

year = "2005",

month = dec,

day = "14",

doi = "10.1021/ja0558544",

language = "English (US)",

volume = "127",

pages = "17182--17183",

journal = "Journal of the American Chemical Society",

issn = "0002-7863",

publisher = "American Chemical Society",

number = "49",

}

TY - JOUR

T1 - Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor

AU - Zheng, Yujun

AU - Balasubramanyam, Karanam

AU - Cebrat, Marek

AU - Buck, Donald

AU - Guidez, Fabien

AU - Zelent, Arthur

AU - Alani, Rhoda M.

AU - Cole, Philip A.

PY - 2005/12/14

Y1 - 2005/12/14

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=29044440879&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=29044440879&partnerID=8YFLogxK

U2 - 10.1021/ja0558544

DO - 10.1021/ja0558544

M3 - Article

C2 - 16332055

AN - SCOPUS:29044440879

VL - 127

SP - 17182

EP - 17183

JO - Journal of the American Chemical Society

JF - Journal of the American Chemical Society

SN - 0002-7863

IS - 49

ER -