Improved inhibition of the histone acetyltransferase PCAF by an anacardic acid derivative

M Ghizzoni, A Boltjes, C de Graaf, HJ Haisma…

Index: Ghizzoni, Massimo; Boltjes, Andre; Graaf, Chris De; Haisma, Hidde J.; Dekker, Frank J. Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 16 p. 5826 - 5834

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Citation Number: 47

Abstract

Several lines of evidence indicate that histone acetyltransferases (HATs) are novel drug targets for treatment of diseases like, for example, cancer and inflammation. The natural product anacardic acid is a starting point for development of small molecule inhibitors of the histone acetyltransferase (HAT) p300/CBP associated factor (PCAF). In order to optimize the inhibitory potency, a binding model for PCAF inhibition by anacardic acid was proposed ...