Targeting Reversible Lysine Modifications

Abstract

Reversible protein lysine modifications including acylation and methylation have been recognized as critical to the regulation of cell growth, differentiation, and gene expression. However, many aspects of their function are poorly understood. We will discuss several chemical approaches that our lab is taking to the functional analysis of lysine acylation and demethylation including inhibitor design strategies and protein semisynthesis. In combination with enzymologic, biophysical, and cellular strategies, these chemical approaches have offered new insights into the roles of lysine post‐ translational modifications in normal and disease states.