Allosteric regulation of epigenetic modifying enzymes.

Allosteric regulation of epigenetic modifying enzymes.
Curr Opin Chem Biol. 2017 Jul 06;39:109-115
Authors: Zucconi BE, Cole PA
Abstract
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.
PMID: 28689145 [PubMed - as supplied by publisher]

Source: Current Opinion in Chemical Biology - July 6, 2017 Category: Biochemistry Authors: Zucconi BE, Cole PA Tags: Curr Opin Chem Biol Source Type: research