Abstract:Protein arginine methyltransferases (PRMTs) catalyse the transfer of methyl groups to arginine residues in proteins. PRMT inhibitors are novel, promising drugs against cancer that are currently in clinical trials, which include oral administration of the drugs. However, off-target activities of systemically available PRMT inhibitorshave not yet been investigated. In this work, we study the relevance of arginine methylation in platelets and investigate the effect of PRMT inhibitors on platelet function and on t… Show more
“…This is important because PRMT inhibitors are in clinical trials, and cross-talk events could lead to possible off-target side effects. Indeed, the monitoring of any side-effects of PRMT inhibitors is a recognised need, 82 in particular in the light of recent investigations of the effect of PRMT inhibitors on platelets 83 and the termination of several clinical trials using PRMT1 inhibitors, including GSK3368715 ( e.g. NCT03666988, NCT03854227).…”
Arginine methylation is a post-translational modification that consists of the transfer of one or two methyl (CH3) groups to arginine residues in proteins. Several types of arginine methylation occur, namely...
“…This is important because PRMT inhibitors are in clinical trials, and cross-talk events could lead to possible off-target side effects. Indeed, the monitoring of any side-effects of PRMT inhibitors is a recognised need, 82 in particular in the light of recent investigations of the effect of PRMT inhibitors on platelets 83 and the termination of several clinical trials using PRMT1 inhibitors, including GSK3368715 ( e.g. NCT03666988, NCT03854227).…”
Arginine methylation is a post-translational modification that consists of the transfer of one or two methyl (CH3) groups to arginine residues in proteins. Several types of arginine methylation occur, namely...
“…60,61 Key platelet proteins are known to be arginine methylated, which may promote aggregation in response to thrombin and collagen. 62 In mouse brain tissue, arginine methylation has been detected in transporters and vesicle proteins as well as in ion channels and receptors, all of which are involved in synaptic transmission. 63…”
Zika virus (ZIKV) and dengue virus (DENV) are two closely related flaviviruses with similar symptoms. However, due to the implications of ZIKV infections for pregnancy outcomes, understanding differences in their...
“…However, epigenetic drugs are increasingly studied in other contexts and developed for treating a range of disorders. Examples published in this collection include the effects of arginine methylation inhibitors on blood platelets, a role for histone kinase inhibitors in neurodegenerative diseases, and the validation of histone deacetylase 8 (HDAC8) inhibitors for the treatment of acute kidney injury . A noteworthy paper focuses on methods for determining cellular target engagement of inhibitors of selected deacetylases …”
Section: Acs Pharmacology and Translational Sciencementioning
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