Literature DB >> 20655754

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

Massimo Ghizzoni1, André Boltjes, Chris de Graaf, Hidde J Haisma, Frank J Dekker.   

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. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20655754     DOI： 10.1016/j.bmc.2010.06.089

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  23 in total

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5.  Glucagon regulates gluconeogenesis through KAT2B- and WDR5-mediated epigenetic effects.

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6.  6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site.

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7.  Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease.

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Journal:  ACS Med Chem Lett       Date:  2019-03-29       Impact factor: 4.345

8.  A functional genomics screen identifies PCAF and ADA3 as regulators of human granzyme B-mediated apoptosis and Bid cleavage.

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Journal:  Cell Death Differ       Date:  2014-01-24       Impact factor: 15.828

9.  Discovery of a novel activator of 5-lipoxygenase from an anacardic acid derived compound collection.

Authors:  Rosalina Wisastra; Petra A M Kok; Nikolaos Eleftheriadis; Matthew P Baumgartner; Carlos J Camacho; Hidde J Haisma; Frank J Dekker
Journal:  Bioorg Med Chem       Date:  2013-10-23       Impact factor: 3.641

10.  Anacardic acid (6-pentadecylsalicylic acid) induces apoptosis of prostate cancer cells through inhibition of androgen receptor and activation of p53 signaling.

Authors:  Jing Tan; Binghai Chen; Leye He; Yuxin Tang; Zhiqiang Jiang; Guangmin Yin; Jinrong Wang; Xianzhen Jiang
Journal:  Chin J Cancer Res       Date:  2012-12       Impact factor: 5.087
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