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Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer.
Liu Q, Chang JW, Wang J, Kang SA, Thoreen CC, Markhard A, Hur W, Zhang J, Sim T, Sabatini DM, Gray NS. Liu Q, et al. J Med Chem. 2010 Oct 14;53(19):7146-55. doi: 10.1021/jm101144f. J Med Chem. 2010. PMID: 20860370 Free PMC article.
Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics.
Liu Q, Kirubakaran S, Hur W, Niepel M, Westover K, Thoreen CC, Wang J, Ni J, Patricelli MP, Vogel K, Riddle S, Waller DL, Traynor R, Sanda T, Zhao Z, Kang SA, Zhao J, Look AT, Sorger PK, Sabatini DM, Gray NS. Liu Q, et al. J Biol Chem. 2012 Mar 23;287(13):9742-9752. doi: 10.1074/jbc.M111.304485. Epub 2012 Jan 5. J Biol Chem. 2012. PMID: 22223645 Free PMC article.
Development of ATP-competitive mTOR inhibitors.
Liu Q, Kang SA, Thoreen CC, Hur W, Wang J, Chang JW, Markhard A, Zhang J, Sim T, Sabatini DM, Gray NS. Liu Q, et al. Methods Mol Biol. 2012;821:447-60. doi: 10.1007/978-1-61779-430-8_29. Methods Mol Biol. 2012. PMID: 22125084 Free PMC article.
Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR.
Liu Q, Xu C, Kirubakaran S, Zhang X, Hur W, Liu Y, Kwiatkowski NP, Wang J, Westover KD, Gao P, Ercan D, Niepel M, Thoreen CC, Kang SA, Patricelli MP, Wang Y, Tupper T, Altabef A, Kawamura H, Held KD, Chou DM, Elledge SJ, Janne PA, Wong KK, Sabatini DM, Gray NS. Liu Q, et al. Among authors: liu y. Cancer Res. 2013 Apr 15;73(8):2574-86. doi: 10.1158/0008-5472.CAN-12-1702. Epub 2013 Feb 22. Cancer Res. 2013. PMID: 23436801 Free PMC article.
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