Allosteric regulation of epigenetic modifying enzymes

Beth E. Zucconi, Philip A. Cole

Research output: Contribution to journalReview article

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.

Original languageEnglish (US)
Pages (from-to)109-115
Number of pages7
JournalCurrent Opinion in Chemical Biology
Volume39
DOIs
StatePublished - Aug 1 2017

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry

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