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- W2912687484 abstract "Epigenetic regulation of gene expression depends on the state of chromatin, which can be modified in a variety of ways, including DNA methylation, nucleosome remodeling histone variants, and posttranslational modifications (PTMs) of histones. Protein methyltransferases (PMTs) are implicated in various cancers and numerous other diseases, and the discovery of selective small-molecule inhibitors of PMTs has become a very active research area. This chapter highlight the progress made in the discovery of PMT inhibitors in the last 15 years. PMTs are classified based on the residues they modify: protein lysine methyltransferases (PKMTs) and protein arginine methyltransferases (PRMTs). The lysine residues can be mono-, di-, and/or trimethylated by PKMTs, and the arginine residues can only be mono- and/or dimethylated by PRMTs. Protein arginine methylation is another significant and widely observed PTM in eukaryotic cells. Every methylation of arginine prevents a potential hydrogen bond, creating steric bulkiness and increasing hydrophobicity." @default.
- W2912687484 created "2019-02-21" @default.
- W2912687484 creator A5011313349 @default.
- W2912687484 creator A5035411478 @default.
- W2912687484 date "2019-02-06" @default.
- W2912687484 modified "2023-09-25" @default.
- W2912687484 title "Selective Small‐Molecule Inhibitors of Protein Methyltransferases" @default.
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- W2912687484 doi "https://doi.org/10.1002/9783527809257.ch9" @default.
- W2912687484 hasPublicationYear "2019" @default.
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