1243583-81-4Relevant articles and documents
Improved inhibition of the histone acetyltransferase PCAF by an anacardic acid derivative
Ghizzoni, Massimo,Boltjes, André,Graaf, Chris De,Haisma, Hidde J.,Dekker, Frank J.
experimental part, p. 5826 - 5834 (2010/10/01)
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.