Inhibition of the PCAF histone acetyl transferase and cell proliferation by isothiazolones

…, M Ghizzoni, N van der Meer, R Wisastra…

Index: Dekker, Frank J.; Ghizzoni, Massimo; van der Meer, Nanette; Wisastra, Rosalina; Haisma, Hidde J. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 2 p. 460 - 466

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Citation Number: 32

Abstract

Small molecule HAT inhibitors are useful tools to unravel the role of histone acetyl transferases (HATs) in the cell and have relevance for oncology. We present a systematic investigation of the inhibition of the HAT p300/CBP Associated Factor (PCAF) by isothiazolones with different substitutions. 5-chloroisothiazolones proved to be the most potent inhibitors of PCAF. The growth inhibition of 4 different cell lines was studied and the ...