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A selective small molecule IkappaB Kinase beta inhibitor blocks nuclear factor kappaB-mediated inflammatory responses in human fibroblast-like synoviocytes, chondrocytes, and mast cells.
Wen D, Nong Y, Morgan JG, Gangurde P, Bielecki A, Dasilva J, Keaveney M, Cheng H, Fraser C, Schopf L, Hepperle M, Harriman G, Jaffee BD, Ocain TD, Xu Y. Wen D, et al. Among authors: cheng h. J Pharmacol Exp Ther. 2006 Jun;317(3):989-1001. doi: 10.1124/jpet.105.097584. Epub 2006 Mar 8. J Pharmacol Exp Ther. 2006. PMID: 16525037
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: cheng h. 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: cheng h. 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.
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: cheng h. Oncotarget. 2014 May 30;5(10):3362-74. doi: 10.18632/oncotarget.1951. Oncotarget. 2014. PMID: 24830942 Free PMC article.
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.
Cho YS, Borland M, Brain C, Chen CH, Cheng H, Chopra R, Chung K, Groarke J, He G, Hou Y, Kim S, Kovats S, Lu Y, O'Reilly M, Shen J, Smith T, Trakshel G, Vögtle M, Xu M, Xu M, Sung MJ. Cho YS, et al. Among authors: cheng h. J Med Chem. 2010 Nov 25;53(22):7938-57. doi: 10.1021/jm100571n. Epub 2010 Nov 1. J Med Chem. 2010. PMID: 21038853
Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling.
Huang SM, Mishina YM, Liu S, Cheung A, Stegmeier F, Michaud GA, Charlat O, Wiellette E, Zhang Y, Wiessner S, Hild M, Shi X, Wilson CJ, Mickanin C, Myer V, Fazal A, Tomlinson R, Serluca F, Shao W, Cheng H, Shultz M, Rau C, Schirle M, Schlegl J, Ghidelli S, Fawell S, Lu C, Curtis D, Kirschner MW, Lengauer C, Finan PM, Tallarico JA, Bouwmeester T, Porter JA, Bauer A, Cong F. Huang SM, et al. Among authors: cheng h. Nature. 2009 Oct 1;461(7264):614-20. doi: 10.1038/nature08356. Epub 2009 Sep 16. Nature. 2009. PMID: 19759537
[1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.
Shultz MD, Kirby CA, Stams T, Chin DN, Blank J, Charlat O, Cheng H, Cheung A, Cong F, Feng Y, Fortin PD, Hood T, Tyagi V, Xu M, Zhang B, Shao W. Shultz MD, et al. Among authors: cheng h. J Med Chem. 2012 Feb 9;55(3):1127-36. doi: 10.1021/jm2011222. Epub 2012 Feb 1. J Med Chem. 2012. PMID: 22260203
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