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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

Protein Lysine Methyltransferases Inhibitors

Author(s): Ying Li, Lei Ding, Shuang Ren, Wen Zhang and Guo-Wu Rao*

Volume 30, Issue 27, 2023

Published on: 14 November, 2022

Page: [3060 - 3089] Pages: 30

DOI: 10.2174/0929867329666220829151257

Price: $65


Protein lysine methylation is a significant protein post-translational modification (PTMs) and has a key function in epigenetic regulation. Protein lysine methyltransferase (PKMTs) mainly catalyzes the lysine methylation of various core histones and a few non-histone proteins. It has been observed that aberrant activity of PKMTs has been found in many cancers and other diseases, and some PKMT inhibitors have been discovered and progressed to clinical trials. This field developed rapidly and has aroused great interest. In this paper, we reviewed the biochemical and biological activities of PKMTs and their association with various cancers. Selective small-molecule inhibitors, including their chemical structure, structure-activity relationship, and in vitro/vivo studies, are also described to provide ideas for the discovery of highly potent, selective PKMT inhibitors.

Keywords: Epigenetics, methylation, protein lysine, methyltransferases, cancer, small molecular, inhibitors.

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FDA FDA granted accelerated approval to tazemetostat for follicular lymphoma. Available from: (Accessed on: 18 June 2020).
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