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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