Changes in protein arginine methylation by GSK3368712
Ontology highlight
ABSTRACT:
INSTRUMENT(S): Orbitrap Fusion Lumos, Q Exactive
ORGANISM(S): Homo Sapiens (human)
TISSUE(S): Pancreatic Adenocarcinoma Cell Line, Leukocyte, Lymph Node
DISEASE(S): Pancreatic Cancer,Lymphoma
SUBMITTER: 
Vicky Yang
LAB HEAD: Helai Mohammad
PROVIDER: PXD012747 | Pride | 2019-09-10
REPOSITORIES: Pride
Publications
Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss.
Fedoriw Andrew A Rajapurkar Satyajit R SR O'Brien Shane S Gerhart Sarah V SV Mitchell Lorna H LH Adams Nicholas D ND Rioux Nathalie N Lingaraj Trupti T Ribich Scott A SA Pappalardi Melissa B MB Shah Niyant N Laraio Jenny J Liu Yan Y Butticello Michael M Carpenter Chris L CL Creasy Caretha C Korenchuk Susan S McCabe Michael T MT McHugh Charles F CF Nagarajan Raman R Wagner Craig C Zappacosta Francesca F Annan Roland R Concha Nestor O NO Thomas Roberta A RA Hart Timothy K TK Smith Jesse J JJ Copeland Robert A RA Moyer Mikel P MP Campbell John J Stickland Kim K Mills James J Jacques-O'Hagan Suzanne S Allain Christina C Johnston Danielle D Raimondi Alejandra A Porter Scott Margaret M Waters Nigel N Swinger Kerren K Boriack-Sjodin Ann A Riera Tom T Shapiro Gideon G Chesworth Richard R Prinjha Rabinder K RK Kruger Ryan G RG Barbash Olena O Mohammad Helai P HP
Cancer cell 20190627 1
Type I protein arginine methyltransferases (PRMTs) catalyze asymmetric dimethylation of arginines on proteins. Type I PRMTs and their substrates have been implicated in human cancers, suggesting inhibition of type I PRMTs may offer a therapeutic approach for oncology. The current report describes GSK3368715 (EPZ019997), a potent, reversible type I PRMT inhibitor with anti-tumor effects in human cancer models. Inhibition of PRMT5, the predominant type II PRMT, produces synergistic cancer cell gro ...[more]
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