Interaction Between DNA/histone Methyltransferases and their Inhibitors

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

Journal Name: Current Medicinal Chemistry

Volume 22 , Issue 3 , 2015

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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.

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

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Article Details

Year: 2015
Published on: 19 December, 2014
Page: [360 - 372]
Pages: 13
DOI: 10.2174/0929867321666141106114538
Price: $65

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