Journal
CURRENT OPINION IN CHEMICAL BIOLOGY
Volume 39, Issue -, Pages 109-115Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.cbpa.2017.05.015
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Funding
- National Institutes of Health [GM62437]
- FAMRI Foundation
- Jane Coffin Childs Memorial Fund
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Epigenetic enzymes including histone modifying enzymes are key regulators of gene expression in normal and disease processes. Many drug development strategies to target histone modifying enzymes have focused on ligands that bind to enzyme active sites, but allosteric pockets offer potentially attractive opportunities for therapeutic development. Recent biochemical studies have revealed roles for small molecule and peptide ligands binding outside of the active sites in modulating the catalytic activities of histone modifying enzymes. Here we highlight several examples of allosteric regulation of epigenetic enzymes and discuss the biological significance of these findings.
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