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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. Among authors: hur w. J Med Chem. 2010 Oct 14;53(19):7146-55. doi: 10.1021/jm101144f. J Med Chem. 2010. PMID: 20860370 Free PMC article.
Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.
Liu Q, Wang J, Kang SA, Thoreen CC, Hur W, Ahmed T, Sabatini DM, Gray NS. Liu Q, et al. Among authors: hur w. J Med Chem. 2011 Mar 10;54(5):1473-80. doi: 10.1021/jm101520v. Epub 2011 Feb 15. J Med Chem. 2011. PMID: 21322566 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. Among authors: hur w. 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.
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. Among authors: hur w. 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.
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: hur w. 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.
Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.
Wang B, Deng Y, Chen Y, Yu K, Wang A, Liang Q, Wang W, Chen C, Wu H, Hu C, Miao W, Hur W, Wang W, Hu Z, Weisberg EL, Wang J, Ren T, Wang Y, Gray NS, Liu Q, Liu J. Wang B, et al. Among authors: hur w. Eur J Med Chem. 2017 Sep 8;137:545-557. doi: 10.1016/j.ejmech.2017.06.016. Epub 2017 Jun 9. Eur J Med Chem. 2017. PMID: 28628824
A structure-guided approach to creating covalent FGFR inhibitors.
Zhou W, Hur W, McDermott U, Dutt A, Xian W, Ficarro SB, Zhang J, Sharma SV, Brugge J, Meyerson M, Settleman J, Gray NS. Zhou W, et al. Among authors: hur w. Chem Biol. 2010 Mar 26;17(3):285-95. doi: 10.1016/j.chembiol.2010.02.007. Chem Biol. 2010. PMID: 20338520 Free PMC article.
230 results