Protein Methylation and Demethylation in Cancer

Abstract

Epigenetic modifications are heritable chromatin alterations that contribute to the temporal and spatial interpretation of the genome. The epigenetic information is conveyed through a multitude of chemical modifications, including DNA methylation, reversible modifications of histones, and ATP-dependent nucleosomal remodeling. Deregulation of the epigenetic machinery contributes to the development of several pathologies, including cancer. During the last decade, we saw an explosion of studies investigating the role of protein methylation/demethylation of histones. Protein methylation and demethylation are catalyzed by protein methyltransferases and protein demethylases. Their substrates have been shown to play important roles in cancers. Although the underlying mechanisms of tumorigenesis are still largely unknown, growing evidence is starting to link aberrant regulation of methylation to tumorigenesis. This review focuses on summarizing the recent progress in understanding of the function of protein lysine and arginine methylation. We also discuss the potential and the caveats of targeting protein methylation for the treatment of cancer.