Researchers have identified a small-molecule inhibitor that may be a valuable tool for gene-repression studies, according to a paper in Nature Chemical Biology’s August issue. Certain disease states, including cancer and neurodegenerative diseases, have been associated with irregularities in gene-repression.
The mature state of a cell is determined by its specific pattern of gene expression, which in turn is established and maintained by how DNA is packaged into DNA-protein bundles, called chromatin. The nucleosome, the basic unit of chromatin, consists of DNA wrapped around four core histone proteins. The addition of methyl groups to histone proteins is known to play an important role in establishing stable gene expression patterns and is coordinated by histone methyltransferase enzymes. Imhof and colleagues have identified from a panel of small molecules a fungal metabolite, chaetocin that specifically inhibits a class of this enzyme responsible for the methylation of histone H3. The authors demonstrate the efficacy of chaetocin both in vitro and in vivo.
Chaetocin could be a powerful tool for studying histone methylation-mediated gene repression, misregulation of which has been associated with various diseases.
Axel Imhof (Ludwig-Maximillians University of Munich, Germany)
Also published online.
(C) Nature Chemical Biology press release.
Message posted by: Trevor M. D'Souza
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