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51 results

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Page 1
Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.
Cohen F, Bergeron P, Blackwood E, Bowman KK, Chen H, Dipasquale AG, Epler JA, Koehler MF, Lau K, Lewis C, Liu L, Ly CQ, Malek S, Nonomiya J, Ortwine DF, Pei Z, Robarge KD, Sideris S, Trinh L, Truong T, Wu J, Zhao X, Lyssikatos JP. Cohen F, et al. Among authors: lyssikatos jp. J Med Chem. 2011 May 12;54(9):3426-35. doi: 10.1021/jm200215y. Epub 2011 Apr 15. J Med Chem. 2011. PMID: 21495671
Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.
Koehler MF, Bergeron P, Blackwood E, Bowman KK, Chen YH, Deshmukh G, Ding X, Epler J, Lau K, Lee L, Liu L, Ly C, Malek S, Nonomiya J, Oeh J, Ortwine DF, Sampath D, Sideris S, Trinh L, Truong T, Wu J, Pei Z, Lyssikatos JP. Koehler MF, et al. Among authors: lyssikatos jp. J Med Chem. 2012 Dec 27;55(24):10958-71. doi: 10.1021/jm301389h. Epub 2012 Dec 12. J Med Chem. 2012. PMID: 23199076
Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).
Estrada AA, Shore DG, Blackwood E, Chen YH, Deshmukh G, Ding X, Dipasquale AG, Epler JA, Friedman LS, Koehler MF, Liu L, Malek S, Nonomiya J, Ortwine DF, Pei Z, Sideris S, St-Jean F, Trinh L, Truong T, Lyssikatos JP. Estrada AA, et al. Among authors: lyssikatos jp. J Med Chem. 2013 Apr 11;56(7):3090-101. doi: 10.1021/jm400194n. Epub 2013 Mar 29. J Med Chem. 2013. PMID: 23473235
Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.
Pei Z, Blackwood E, Liu L, Malek S, Belvin M, Koehler MF, Ortwine DF, Chen H, Cohen F, Kenny JR, Bergeron P, Lau K, Ly C, Zhao X, Estrada AA, Truong T, Epler JA, Nonomiya J, Trinh L, Sideris S, Lesnick J, Bao L, Vijapurkar U, Mukadam S, Tay S, Deshmukh G, Chen YH, Ding X, Friedman LS, Lyssikatos JP. Pei Z, et al. Among authors: lyssikatos jp. ACS Med Chem Lett. 2012 Nov 29;4(1):103-7. doi: 10.1021/ml3003132. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900569 Free PMC article.
Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1.
Gazzard L, Appleton B, Chapman K, Chen H, Clark K, Drobnick J, Goodacre S, Halladay J, Lyssikatos J, Schmidt S, Sideris S, Wiesmann C, Williams K, Wu P, Yen I, Malek S. Gazzard L, et al. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5704-5709. doi: 10.1016/j.bmcl.2014.10.063. Epub 2014 Oct 27. Bioorg Med Chem Lett. 2014. PMID: 25453805
Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.
Hu H, Wang X, Chan GK, Chang JH, Do S, Drummond J, Ebens A, Lee W, Ly J, Lyssikatos JP, Murray J, Moffat JG, Chao Q, Tsui V, Wallweber H, Kolesnikov A. Hu H, et al. Among authors: lyssikatos jp. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5258-64. doi: 10.1016/j.bmcl.2015.09.052. Epub 2015 Sep 30. Bioorg Med Chem Lett. 2015. PMID: 26459208
Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.
Zak M, Hanan EJ, Lupardus P, Brown DG, Robinson C, Siu M, Lyssikatos JP, Romero FA, Zhao G, Kellar T, Mendonca R, Ray NC, Goodacre SC, Crackett PH, McLean N, Hurley CA, Yuen PW, Cheng YX, Liu X, Liimatta M, Kohli PB, Nonomiya J, Salmon G, Buckley G, Lloyd J, Gibbons P, Ghilardi N, Kenny JR, Johnson A. Zak M, et al. Among authors: lyssikatos jp. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1522-1531. doi: 10.1016/j.bmcl.2019.04.008. Epub 2019 Apr 4. Bioorg Med Chem Lett. 2019. PMID: 30981576
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.
Hanan EJ, van Abbema A, Barrett K, Blair WS, Blaney J, Chang C, Eigenbrot C, Flynn S, Gibbons P, Hurley CA, Kenny JR, Kulagowski J, Lee L, Magnuson SR, Morris C, Murray J, Pastor RM, Rawson T, Siu M, Ultsch M, Zhou A, Sampath D, Lyssikatos JP. Hanan EJ, et al. Among authors: lyssikatos jp. J Med Chem. 2012 Nov 26;55(22):10090-107. doi: 10.1021/jm3012239. Epub 2012 Oct 24. J Med Chem. 2012. PMID: 23061660
Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.
Liang J, van Abbema A, Balazs M, Barrett K, Berezhkovsky L, Blair W, Chang C, Delarosa D, DeVoss J, Driscoll J, Eigenbrot C, Ghilardi N, Gibbons P, Halladay J, Johnson A, Kohli PB, Lai Y, Liu Y, Lyssikatos J, Mantik P, Menghrajani K, Murray J, Peng I, Sambrone A, Shia S, Shin Y, Smith J, Sohn S, Tsui V, Ultsch M, Wu LC, Xiao Y, Yang W, Young J, Zhang B, Zhu BY, Magnuson S. Liang J, et al. J Med Chem. 2013 Jun 13;56(11):4521-36. doi: 10.1021/jm400266t. Epub 2013 May 29. J Med Chem. 2013. PMID: 23668484
51 results