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Papers In Press, published online ahead of print March 6, 2003
Molecular Biology and Genetics Unit, Jawaharlal Nehru Centre for Advanced Scientific Research, Bangalore, Karnataka 560064
Corresponding Author: tapas{at}jncasr.ac.in
Histone acetyltransferases (HATs) are a group of enzymes, which play a significant role in the regulation of gene expression. These enzymes covalently modify the N-terminal lysine residues of histones by the addition of acetyl groups from acetyl-CoA. Dysfunction of these enzymes is often associated with the manifestation of several diseases, predominantly cancer. Here we report that anacardic acid (AA) from Cashew Nut Shell Liquid (CNSL) is a potent inhibitor of p300 and PCAF histone acetyltranferase activities. Though it does not affect DNA transcription, HAT-dependent transcription from a chromatin template was strongly inhibited by AA. Furthermore, we describe the design and synthesis of an amide derivative N- (4-Chloro-3- trifluoromethyl-phenyl)-2-ethoxy-6-pentadecyl-benzamide (CTPB) using anacardic acid as a synthon, which remarkably activates p300 HAT activity but not that of PCAF. Though CTPB does not affect DNA-transcription, it enhances the p300 HAT dependent transcriptional activation from in vitro assembled chromatin template. However, it has no effect on histone deacetylase activity. These compounds would be useful as biological switching molecules for probing into the role of p300 in transcriptional studies and may also be useful as new chemical entities for the development of anticancer drugs.
J. Biol. Chem, 10.1074/jbc.M301580200
Submitted on February 13, 2003
Revised on March 6, 2003
Accepted on March 6, 2003
Small molecule modulators of histone acetyltransferase p300
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