期刊
JOURNAL OF CELLULAR BIOCHEMISTRY
卷 116, 期 8, 页码 1595-1601出版社
WILEY-BLACKWELL
DOI: 10.1002/jcb.25113
关键词
ANTI-CANCER; p68 RNA HELICASE; PHOSPHO-p68; RX-5902
资金
- National Institute of Health [CA118113]
- Georgia Cancer Coalition
- Center of Diagnosis Therapeutics
1-(3,5-Dimethoxyphenyl)-4-[(6-fluoro-2-methoxyquinoxalin-3-yl)aminocarbonyl] piperazine (RX-5902) exhibits strong growth inhibition in various human cancer cell lines with IC50 values ranging between 10 and 20nM. In this study, we demonstrate that p68 RNA helicase is a cellular target of RX-5902 by the drug affinity responsive target stability (DARTS) method, and confirmed the direct binding of H-3-labeled RX-5902 to Y593 phospho-p68 RNA helicase. We further demonstrated RX-5902 inhibited the -catenin dependent ATPase activity of p68 RNA helicase in an in vitro system. Furthermore, we showed that treatment of cancer cells with RX-5902 resulted in the downregulation of the expression of certain genes, which are known to be regulated by the -catenin pathway, such as c-Myc, cyclin D1 and p-c-Jun. Therefore, our study indicates that the inhibition of Y593 phospho-p68 helicase - -catenin interaction by direct binding of RX-5902 to Y593 phospho-p68 RNA helicase may contribute to the anti-cancer activity of this compound. J. Cell. Biochem. 116: 1595-1601, 2015. (c) 2015 Wiley Periodicals, Inc.
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