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First-in-Class Phosphorylated-p68 Inhibitor RX-5902 Inhibits β-Catenin Signaling and Demonstrates Antitumor Activity in Triple-Negative Breast Cancer.
Capasso A, Bagby SM, Dailey KL, Currimjee N, Yacob BW, Ionkina A, Frank JG, Kim DJ, George C, Lee YB, Benaim E, Gittleman B, Hartman SJ, Tan AC, Kim J, Pitts TM, Eckhardt SG, Tentler JJ, Diamond JR. Capasso A, et al. Mol Cancer Ther. 2019 Nov;18(11):1916-1925. doi: 10.1158/1535-7163.MCT-18-1334. Epub 2019 Sep 5. Mol Cancer Ther. 2019. PMID: 31488700 Free PMC article.
RX-5902 was active in vivo against TNBC PDX models, and treatment resulted in a decrease in nuclear β-catenin. RX-5902 exhibited dose-proportional pharmacokinetics and plasma and tumor tissue in nude mice. ...This study supports the continued investiga
RX-5902 was active in vivo against TNBC PDX models, and treatment resulted in a decrease in nuclear β-catenin. RX-59
Structural characterization of β-catenin and RX-5902 binding to phospho-p68 RNA helicase by molecular dynamics simulation.
Ali W, Shafique S, Rashid S. Ali W, et al. Prog Biophys Mol Biol. 2018 Dec;140:79-89. doi: 10.1016/j.pbiomolbio.2018.04.011. Epub 2018 May 2. Prog Biophys Mol Biol. 2018. PMID: 29729328
Evidently, transactivation and C-terminal helicase domains of phospho-p68 exhibited dramatic conformational alterations to assist β-catenin and RX-5902 binding. ...Clearly, the comparative docking-for-functional analysis of phospho-p68 against RX-5902
Evidently, transactivation and C-terminal helicase domains of phospho-p68 exhibited dramatic conformational alterations to assist β-catenin …
A Novel Anti-Cancer Agent, 1-(3,5-Dimethoxyphenyl)-4-[(6-Fluoro-2-Methoxyquinoxalin-3-yl)Aminocarbonyl] Piperazine (RX-5902), Interferes With β-Catenin Function Through Y593 Phospho-p68 RNA Helicase.
Kost GC, Yang MY, Li L, Zhang Y, Liu CY, Kim DJ, Ahn CH, Lee YB, Liu ZR. Kost GC, et al. J Cell Biochem. 2015 Aug;116(8):1595-601. doi: 10.1002/jcb.25113. J Cell Biochem. 2015. PMID: 25649741
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 (3) H-labeled RX-5902 to Y593 phospho-p68 RNA helicase. We further …
In this study, we demonstrate that p68 RNA helicase is a cellular target of RX-5902 by the drug affinity responsive target sta …
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