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ID: ALA1212875
Journal: Bioorg Med Chem
Title: Improved inhibition of the histone acetyltransferase PCAF by an anacardic acid derivative.
Authors: Ghizzoni M, Boltjes A, Graaf Cd, Haisma HJ, Dekker FJ.
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 and new anacardic acid derivatives were designed. Ten new derivatives were synthesized using a novel synthetic route. One compound showed a twofold improved inhibitory potency for the PCAF HAT activity and a twofold improved inhibition of histone acetylation in HEP G2 cells.
CiteXplore: 20655754