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Discovery of SARxxxx92, a pan-PIM kinase inhibitor, efficacious in a KG1 tumor model.
Barberis C, Erdman P, Czekaj M, Fire L, Pribish J, Tserlin E, Maniar S, Batchelor JD, Liu J, Patel VF, Hebert A, Levit M, Wang A, Sun F, Huang SA. Barberis C, et al. Bioorg Med Chem Lett. 2020 Dec 1;30(23):127625. doi: 10.1016/j.bmcl.2020.127625. Epub 2020 Oct 20. Bioorg Med Chem Lett. 2020. PMID: 33096160
Combination of PIM and JAK2 inhibitors synergistically suppresses MPN cell proliferation and overcomes drug resistance.
Huang SM, Wang A, Greco R, Li Z, Barberis C, Tabart M, Patel V, Schio L, Hurley R, Chen B, Cheng H, Lengauer C, Pollard J, Watters J, Garcia-Echeverria C, Wiederschain D, Adrian F, Zhang J. Huang SM, et al. Among authors: patel v. Oncotarget. 2014 May 30;5(10):3362-74. doi: 10.18632/oncotarget.1951. Oncotarget. 2014. PMID: 24830942 Free PMC article.
PIM inhibitors target CD25-positive AML cells through concomitant suppression of STAT5 activation and degradation of MYC oncogene.
Guo Z, Wang A, Zhang W, Levit M, Gao Q, Barberis C, Tabart M, Zhang J, Hoffmann D, Wiederschain D, Rocnik J, Sun F, Murtie J, Lengauer C, Gross S, Zhang B, Cheng H, Patel V, Schio L, Adrian F, Dorsch M, Garcia-Echeverria C, Huang SM. Guo Z, et al. Among authors: patel v. Blood. 2014 Sep 11;124(11):1777-89. doi: 10.1182/blood-2014-01-551234. Epub 2014 Jul 8. Blood. 2014. PMID: 25006129 Free article. Clinical Trial.
Evaluation of cancer dependence and druggability of PRP4 kinase using cellular, biochemical, and structural approaches.
Gao Q, Mechin I, Kothari N, Guo Z, Deng G, Haas K, McManus J, Hoffmann D, Wang A, Wiederschain D, Rocnik J, Czechtizky W, Chen X, McLean L, Arlt H, Harper D, Liu F, Majid T, Patel V, Lengauer C, Garcia-Echeverria C, Zhang B, Cheng H, Dorsch M, Huang SA. Gao Q, et al. Among authors: patel v. J Biol Chem. 2013 Oct 18;288(42):30125-30138. doi: 10.1074/jbc.M113.473348. Epub 2013 Sep 3. J Biol Chem. 2013. PMID: 24003220 Free PMC article.
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.
Harmange JC, Weiss MM, Germain J, Polverino AJ, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, DiPietro L, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Martin MW, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Wang L, White RD, Whittington DA, Zanon R. Harmange JC, et al. J Med Chem. 2008 Mar 27;51(6):1649-67. doi: 10.1021/jm701097z. Epub 2008 Mar 7. J Med Chem. 2008. PMID: 18324761
Discovery of N-(4-(3-(2-aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), a highly selective, orally bioavailable inhibitor of aurora kinases with activity against multidrug-resistant cancer cell lines.
Geuns-Meyer S, Cee VJ, Deak HL, Du B, Hodous BL, Nguyen HN, Olivieri PR, Schenkel LB, Vaida KR, Andrews P, Bak A, Be X, Beltran PJ, Bush TL, Chaves MK, Chung G, Dai Y, Eden P, Hanestad K, Huang L, Lin MH, Tang J, Ziegler B, Radinsky R, Kendall R, Patel VF, Payton M. Geuns-Meyer S, et al. J Med Chem. 2015 Jul 9;58(13):5189-207. doi: 10.1021/acs.jmedchem.5b00183. Epub 2015 May 31. J Med Chem. 2015. PMID: 25970324
6,151 results