Article
Strategy for "detoxification" of a cancer-derived histone mutant based on mapping its interaction with the methyltransferase PRC2.
Journal of the American Chemical Society - 1 Oct 2014
Brown Zachary Z, Müller Manuel M, Jain Siddhant U, Allis C David, Lewis Peter W, Muir Tom W
Abstract excerpt
The histone methyltransferase PRC2 plays a central role in genomic stability and cellular development. Consequently, its misregulation has been implicated in several cancers. Recent work has shown that a histone H3 mutant, where the PRC2 substrate residue Lys27 is replaced by methionine, is also associated with cancer phenotypes and functions as an inhibitor of PRC2. Here we investigate the mechanism of this PRC2...
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