Tag: PRMT

DS-437 is a Dual PRMT5/7 Inhibitor

Protein arginine methyltransferases are a class of enzymes. They transfer a methyl group from the cofactor S-adenosylmethionine (SAM) onto the arginine omega nitrogens of substrate proteins, including histones. There are three subclasses based on their product specificity: type I, II, and III PRMTs asymmetrically dimethylate, symmetrically dimethylate, and monomethylate their...

DW14800, a PRMT5 Inhibitor, Promotes HNF4α Transcription.

Nowadays, liver cancer becomes more frequent among various kinds of diseases. There are many factors leading to liver cancer, such as hepatitis B, hepatitis C or alcohol. Except for these, non-alcoholic fatty liver disease and liver flukes may cause liver cancer. Cancer stem cells (CSCs) are cancer cells, with...

GSK3368715 is an Orally Active Type I PRMT Inhibitor

GSK3368715 is an orally active type I PRMT inhibitor. Protein arginine methyltransferases (PRMTs) transfer a methyl group from S-adenosyl-L-methionine (SAM) to the substrate arginine side chain. All PRMTs can generate ω-NG-monomethyl-arginine (MMA) through a single methylation event. However, type I and II enzymes catalyze progression from MMA to NG-asymmetric...

MS023 is a Selective Inhibitor of Human Type I Protein Arginine Methyltransferases

Protein arginine methyltransferases (PRMTs) play a crucial role in a variety of biological processes. PRMTs divide into three categories. Firstly, type I PRMTs catalyzes mono- and asymmetric dimethylation of arginine residues. Secondly, type II PRMTs catalyzes mono- and symmetric dimethylation of arginine residues. Finally, type III PRMT catalyzes only...

JNJ-64619178 is a Selective PRMT5 Inhibitor with Potent Activity In Lung Cancer

Protein arginine methylation, a common post-translational modification, involves in numerous cellular processes including transcription, DNA repair, mRNA splicing and signal transduction. Protein arginine methyltransferases (PRMTs) catalyze arginine methylation on both chromatin-bound and cytoplasmic proteins. Currently, there are nine protein arginine methyltransferases (PRMTs) encoded in mammalian genomes. Each PRMT isoform...

Role of PRMT7 Probe SGC3027 in Cancer

Protein arginine methyltransferases (PRMTs) transfer methyl groups to the arginine residues of histones and other proteins. Fistly, PRMTs add one or two mono-methyl groups to the guanidino nitrogen atoms of arginine residues. And secondly, PRMTs results in epigenetic modification of histones or changes of protein-protein interactions. Lastly, these interactions...