Interaction Between DNA/histone Methyltransferases and their Inhibitors

Title:Interaction Between DNA/histone Methyltransferases and their Inhibitors

Volume: 22 Issue: 3

Author(s): J. Hu, S. Chen, X. Kong, K. Zhu, S. Cheng, M. Zheng, H. Jiang and C. Luo

Affiliation:

• Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.,China

Keywords: DNA methyltransferase, drug discovery, epigenetic therapy, histone methyltransferase, inhibitor.

Abstract: Epigenetic research has recently become one of the hotspots in the field of bioscience and drug design. DNA methylation and histone methylation serve a critical function in influencing gene expression and genome function. The inhibition of DNA and histone methyltransferases (DNMTs and HMTs) is a promising approach for the therapeutic treatment of numerous diseases, including cancer. This work reviews the recent achievements in methyltransferase crystallographic structure resolution and bioactive inhibitor screening. We discuss the features of DNA and HMT structures, as well as the mechanism and structure–function relationship of transferase inhibitors, to elucidate how methyltransferase and inhibitor interactions occur both internally and externally. This study briefly reviews the biological function, as well as the inhibitor discovery and development, of DNA/histone methyltransferases.

Cite this article as:

Hu J., Chen S., Kong X., Zhu K., Cheng S., Zheng M., Jiang H. and Luo C., Interaction Between DNA/histone Methyltransferases and their Inhibitors, Current Medicinal Chemistry 2015; 22(3) . https://dx.doi.org/10.2174/0929867321666141106114538