Turning Nonselective Inhibitors of Type I Protein Arginine Methyltransferases into Potent and Selective Inhibitors of Protein Arginine Methyltransferase 4 through a Deconstruction–Reconstruction and Fragment-Growing Approach
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DOI: 10.1021/acs.jmedchem.2c00252
Abstract: Protein arginine methyltransferases (PRMTs) are important therapeutic targets, playing a crucial role in the regulation of many cellular processes and being linked to many diseases. Yet, there is still much to be understood regarding their… read more here.
Keywords: protein arginine; arginine; selective inhibitors; deconstruction reconstruction ... See more keywords
Functional Study of Leishmania braziliensis Protein Arginine Methyltransferases (PRMTs) Reveals That PRMT1 and PRMT5 Are Required for Macrophage Infection.
Sign Up to like & getrecommendations! Published in 2022 at "ACS infectious diseases"
DOI: 10.1021/acsinfecdis.1c00509
Abstract: In trypanosomatids, regulation of gene expression occurs mainly at the posttranscriptional level, and RNA-binding proteins (RBPs) are key players in determining the fates of transcripts. RBPs are targets of protein arginine methyltransferases (PRMTs), which posttranslationally… read more here.
Keywords: methylation; protein arginine; methyltransferases prmts; braziliensis ... See more keywords
Structural and biochemical evaluation of bisubstrate inhibitors of protein arginine N-methyltransferases PRMT1 and CARM1 (PRMT4)
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DOI: 10.1042/bcj20190826
Abstract: Attenuating the function of protein arginine methyltransferases (PRMTs) is an objective for the investigation and treatment of several diseases including cardiovascular disease and cancer. Bisubstrate inhibitors that simultaneously target binding sites for arginine substrate and… read more here.
Keywords: protein arginine; evaluation bisubstrate; bisubstrate; arginine methyltransferases ... See more keywords
The role of protein arginine methyltransferases in pathogenesis and treatment of digestive system carcinoma.
Sign Up to like & getrecommendations! Published in 2023 at "Molecular cancer therapeutics"
DOI: 10.1158/1535-7163.mct-22-0746
Abstract: Post-translational modification of proteins increases their diversity and maintains the stability of the intracellular environment. Protein arginine methyltransferases (PRMTs) are an important family of epigenetic modification enzymes, which play a critical role in post-translational modification.… read more here.
Keywords: protein arginine; role; digestive system; arginine methyltransferases ... See more keywords
Structural and biochemical evaluation of bisubstrate inhibitors of protein arginine N-methyltransferases PRMT1 and CARM1 (PRMT4).
Sign Up to like & getrecommendations! Published in 2020 at "Biochemical Journal"
DOI: 10.2210/pdb6s7c/pdb
Abstract: Attenuating the function of protein arginine methyltransferases (PRMTs) is an objective for the investigation and treatment of several diseases including cardiovascular disease and cancer. Bisubstrate inhibitors that simultaneously target binding sites for arginine substrate and… read more here.
Keywords: protein arginine; evaluation bisubstrate; bisubstrate; arginine methyltransferases ... See more keywords
Protein arginine methyltransferases in renal development, injury, repair, and fibrosis
Sign Up to like & getrecommendations! Published in 2023 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2023.1123415
Abstract: Protein arginine methyltransferases (PRMTs) methylate a range of histone and non-histone substrates and participate in multiple biological processes by regulating gene transcription and post-translational modifications. To date, most studies on PRMTs have focused on their… read more here.
Keywords: protein arginine; repair fibrosis; arginine methyltransferases; development injury ... See more keywords
The Role of Protein Arginine Methyltransferases in DNA Damage Response
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DOI: 10.3390/ijms23179780
Abstract: In response to DNA damage, cells have developed a sophisticated signaling pathway, consisting of DNA damage sensors, transducers, and effectors, to ensure efficient and proper repair of damaged DNA. During this process, posttranslational modifications (PTMs)… read more here.
Keywords: protein arginine; damage; dna damage; arginine methyltransferases ... See more keywords