Among the different epigenetic target families, protein lysine methyltransferases (PKMTs), are especially interesting because it is believed that their inhibition may be highly specific at the functional level. Despite its relevance, there are currently known inhibitors against only 10 out of the 50 ...
Protein lysine methylation is a crucial post-translational modification that regulates the functions of both histone and non-histone proteins. Deregulation of the enzymes or ‘writers’ of protein lysine methylation, lysine methyltransferases (KMTs), is
Protein lysine methyltransferases (PKMTs) play crucial roles in histone and nonhistone modifications, and their dysregulation has been linked to the development and progression of cancer. While the majority of studies have focused on the oncogenic functi
PKMT inhibitors: a double-edged sword in cancer treatment The review summarizes the tumor-suppressive role of protein lysine methyltransferases (PKMTs), a group of enzymes that add a methyl group to the lysine residues of proteins. The authors highlight three PKMTs – SETD2, SETD7, and ...
The protein methyltransferases (PMTs) represent a large class of enzymes that catalyse the methylation of side chain nitrogen atoms of the amino acids lysine or arginine at specific locations along the primary sequence of target proteins. These enzymes play a key role in the spatio-temporal control...
two years tremendous progress has been made in the discovery of selective,small moleculeinhibitors of protein lysine and arginine methyltransferases. Inhibitors of PMTs have been used extensively in oncology studies as tool compounds, and inhibitors ofEZH2,DOT1Land PRMT5 are currently inclinical ...
G9a-like protein (GLP) and G9a are highly homologous protein lysine methyltransferases (PKMTs) sharing approximately 80% sequence identity in their catalytic domains. GLP and G9a form a heterodimer complex and catalyze mono- and dimethylation of histone H3 lysine 9 and nonhistone substrates. Alth...
Lysine methyltransferase inhibitors: where we are now RSC Chem. Biol., 3 (4) (2022), pp. 359-406 10.1039/D1CB00196E CrossrefGoogle Scholar 7. Hwang J. W., Cho Y., Bae G.-U., Kim S.-N., Kim Y. K. Protein arginine methyltransferases: promising targets for cancer therapy Exp. ...
2019). Based on the substrates involved, protein methyltransferases can be divided into categories such as protein lysine methyltransferases (PKMTs) and protein arginine methyltransferases (PRMTs) (Bhat et al. 2021; Dai et al. 2021; Xu and Richard 2021). PKMTs can cause monomethylation, bi...
The crystal structures of the ternary complexes of SET7/9 [21] and DIM-5 [16], respectively bound to AdoHcy and histone H3 peptides have yielded insights into the catalytic mechanism of the SET-domain methyltransferases. In both proteins, the walls of the lysine-binding channel are formed ...