| Literature DB >> 26101569 |
Lorna H Mitchell1, Allison E Drew1, Scott A Ribich1, Nathalie Rioux1, Kerren K Swinger1, Suzanne L Jacques1, Trupti Lingaraj1, P Ann Boriack-Sjodin1, Nigel J Waters1, Tim J Wigle1, Oscar Moradei1, Lei Jin1, Tom Riera1, Margaret Porter-Scott1, Mikel P Moyer1, Jesse J Smith1, Richard Chesworth1, Robert A Copeland1.
Abstract
A novel aryl pyrazole series of arginine methyltransferase inhibitors has been identified. Synthesis of analogues within this series yielded the first potent, selective, small molecule PRMT6 inhibitor tool compound, EPZ020411. PRMT6 overexpression has been reported in several cancer types suggesting that inhibition of PRMT6 activity may have therapeutic utility. Identification of EPZ020411 provides the field with the first small molecule tool compound for target validation studies. EPZ020411 shows good bioavailability following subcutaneous dosing in rats making it a suitable tool for in vivo studies.Entities:
Keywords: PRMT6; oncology; protein methyltransferase; tool compound
Year: 2015 PMID： 26101569 PMCID： PMC4468411 DOI： 10.1021/acsmedchemlett.5b00071
Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345