Abstract

Development of JmjC Histone Demethylase Inhibitors

Akane Kawamura, Research Fellow, University Of Oxford

Post-translational modifications on histone tails are important in epigenetic regulation of gene expression. N-methylation on lysine residues is removed by histone demethylases (KDMs). JmjC-domain containing KDMs are Fe(II) and 2-oxoglutarate dependent oxygenases, which make up the larger of the two KDM families. This talk will give an overview of our recent inhibitor development efforts for this family of enzymes, including new strategies used to develop histone substrate competitive cyclic peptide inhibitors for the KDM4A-C.