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AuthorSmith E.
AuthorZhou W.
AuthorShindiapina P.
AuthorSif S.
AuthorLi C.
AuthorBaiocchi R.A.
Available date2019-09-25T11:18:31Z
Publication Date2018
Publication NameExpert Opinion on Therapeutic Targets
ResourceScopus
ISSN14728222
URIhttp://dx.doi.org/10.1080/14728222.2018.1474203
URIhttp://hdl.handle.net/10576/11944
AbstractIntroduction: Exploration in the field of epigenetics has revealed the diverse roles of the protein arginine methyltransferase (PRMT) family of proteins in multiple disease states. These findings have led to the development of specific inhibitors and discovery of several new classes of drugs with potential to treat both benign and malignant conditions. Areas covered: We provide an overview on the role of PRMT enzymes in healthy and malignant cells, highlighting the role of arginine methylation in specific pathways relevant to cancer pathogenesis. Additionally, we describe structure and catalytic activity of PRMT and discuss the mechanisms of action of novel small molecule inhibitors of specific members of the arginine methyltransferase family. Expert opinion: As the field of PRMT biology advances, it’s becoming clear that this class of enzymes is highly relevant to maintaining normal physiologic processes as well and disease pathogenesis. We discuss the potential impact of PRMT inhibitors as a broad class of drugs, including the pleiotropic effects, off target effects the need for more detailed PRMT-centric interactomes, and finally, the potential for targeting this class of enzymes in clinical development of experimental therapeutics for cancer. © 2018, © 2018 Informa UK Limited, trading as Taylor & Francis Group.
SponsorThe study was funded by the Qatar National Research Fund (QNRF) through the National Priorities Research Program (NPRP) grant [NPRP8-617-3-131].
Languageen
PublisherTaylor and Francis Ltd
Subjectarginine-methylation
Cancer
epigenetics
therapeutic target
TitleRecent advances in targeting protein arginine methyltransferase enzymes in cancer therapy
TypeArticle Review
Pagination527-545
Issue Number6
Volume Number22
dc.accessType Open Access


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