Dysregulation of protein methyltransferases in human cancer: An emerging target class for anticancer therapy

By Ryuji Hamamoto, Yusuke Nakamura. 2016

80 citations recorded by the source corpus.

Protein methylation is one of the important post‐translational modifications. Although its biological and physiological functions were unknown for a long time, we and others have characterized a number of protein methyltransferases, which have unveiled the critical functions of protein methylation in various cellular processes, in particular, in epigenetic regulation. In addition, it had been believed that protein methylation is an irreversible phenomenon, but through identification of a variety of protein demethylases, protein methylation is now considered to be dynamically regulated similar to protein phosphorylation. A large amount of evidence indicated that protein methylation has a pivotal role in post‐translational modification of histone proteins as well as non‐histone proteins and is involved in various processes of cancer development and progression. As dysregulation of this modification has been observed frequently in various types of cancer, small‐molecule inhibitors targeting protein methyltransferases and demethylases have been actively developed as anticancer drugs; clinical trials for some of these drugs have already begun. In this review, we discuss the biological and physiological importance of protein methylation in human cancer, especially focusing on the significance of protein methyltransferases as emerging targets for anticancer therapy.

Subfields: Molecular Biology

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Citations in the corpus

Novel prognostic marker PRMT1 regulates cell growth via downregulation of CDKN1A in HCC (2017, background): “Various studies have also reported the overexpression of histone methyltransferases/demethylases in HCC, such as SMYD2/3 [19], SUV39H1/2, G9a and Dot1L [20].”
Critical roles of SMYD2-mediated β-catenin methylation for nuclear translocation and activation of Wnt signaling (2017, background): “Since it is known that the majority of SMYD2 protein is located in the cytoplasm, we hypothesized that methylation of a lysine residue in β-catenin might affect its subcellular localization in cancer cells as we reported examples in our review [10, 11] and in turn, regulate the Wnt signaling pathway”
Epigenetics Analysis and Integrated Analysis of Multiomics Data, Including Epigenetic Data, Using Artificial Intelligence in the Era of Precision Medicine (2019, background): “phosphorylation and sumoylation and non-coding RNAs [15,20,21].”