title: Targeting protein arginine N-methyltransferases with peptide-based inhibitors: opportunities and challenges.
abstract: Recently peptide-based inhibitors have been used to selectively inhibit a family of epigenetic enzymes called protein arginine N-methyltransferases (PRMTs), which has been implicated in different physiological processes and human diseases, such as heart disease and cancer. The diverse efforts to tease out subtle structural differences among PRMT enzymes in order to generate selective inhibitors as well as existing challenges in the field will be examined. The acquisition of PRMT substrate sequence preferences and structural information obtained from small-molecule inhibitors have helped in developing different peptide-based inhibitors that show great promise not only as inhibitors, but also as molecular probes to characterize PRMTs.
authors.affiliation: Faculty of Pharmaceutical Sciences, The University of British Columbia, 2405 Wesbrook Mall, Vancouver, British Columbia, V6T 1Z3, Canada.
authors.forename: Mynol
authors.initials: M
authors.lastname: Vhuiyan
authors.forename: Dylan
authors.initials: D
authors.lastname: Thomas
authors.forename: Farhad
authors.initials: F
authors.lastname: Hossen
authors.forename: Adam
authors.initials: A
authors.lastname: Frankel
mesh_terms: D010455:Peptides / Q000494:pharmacology*; D011484:Protein-Arginine N-Methyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013379:Substrate Specificity
chemical_list: D010455:Peptides; D011484:Protein-Arginine N-Methyltransferases