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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
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.
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.
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.
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
Selective inhibition of mutant isocitrate dehydrogenase 1 (IDH1) via disruption of a metal binding network by an allosteric small molecule.
Deng G, Shen J, Yin M, McManus J, Mathieu M, Gee P, He T, Shi C, Bedel O, McLean LR, Le-Strat F, Zhang Y, Marquette JP, Gao Q, Zhang B, Rak A, Hoffmann D, Rooney E, Vassort A, Englaro W, Li Y, Patel V, Adrian F, Gross S, Wiederschain D, Cheng H, Licht S. Deng G, et al. Among authors: cheng h. J Biol Chem. 2015 Jan 9;290(2):762-74. doi: 10.1074/jbc.M114.608497. Epub 2014 Nov 12. J Biol Chem. 2015. PMID: 25391653 Free PMC article.
Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.
Cho YS, Angove H, Brain C, Chen CH, Cheng H, Cheng R, Chopra R, Chung K, Congreve M, Dagostin C, Davis DJ, Feltell R, Giraldes J, Hiscock SD, Kim S, Kovats S, Lagu B, Lewry K, Loo A, Lu Y, Luzzio M, Maniara W, McMenamin R, Mortenson PN, Benning R, O'Reilly M, Rees DC, Shen J, Smith T, Wang Y, Williams G, Woolford AJ, Wrona W, Xu M, Yang F, Howard S. Cho YS, et al. Among authors: cheng h, cheng r. ACS Med Chem Lett. 2012 May 17;3(6):445-9. doi: 10.1021/ml200241a. eCollection 2012 Jun 14. ACS Med Chem Lett. 2012. PMID: 24900493 Free PMC article.
Dependence on the Pyrimidine Biosynthetic Enzyme DHODH Is a Synthetic Lethal Vulnerability in Mutant KRAS-Driven Cancers.
Koundinya M, Sudhalter J, Courjaud A, Lionne B, Touyer G, Bonnet L, Menguy I, Schreiber I, Perrault C, Vougier S, Benhamou B, Zhang B, He T, Gao Q, Gee P, Simard D, Castaldi MP, Tomlinson R, Reiling S, Barrague M, Newcombe R, Cao H, Wang Y, Sun F, Murtie J, Munson M, Yang E, Harper D, Bouaboula M, Pollard J, Grepin C, Garcia-Echeverria C, Cheng H, Adrian F, Winter C, Licht S, Cornella-Taracido I, Arrebola R, Morris A. Koundinya M, et al. Among authors: cheng h. Cell Chem Biol. 2018 Jun 21;25(6):705-717.e11. doi: 10.1016/j.chembiol.2018.03.005. Epub 2018 Apr 5. Cell Chem Biol. 2018. PMID: 29628435 Free article.
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