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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.
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
[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
Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer.
El-Ahmad Y, Tabart M, Halley F, Certal V, Thompson F, Filoche-Rommé B, Gruss-Leleu F, Muller C, Brollo M, Fabien L, Loyau V, Bertin L, Richepin P, Pilorge F, Desmazeau P, Girardet C, Beccari S, Louboutin A, Lebourg G, Le-Roux J, Terrier C, Vallée F, Steier V, Mathieu M, Rak A, Abecassis PY, Vicat P, Benard T, Bouaboula M, Sun F, Shomali M, Hebert A, Levit M, Cheng H, Courjaud A, Ginesty C, Perrault C, Garcia-Echeverria C, McCort G, Schio L. El-Ahmad Y, et al. Among authors: cheng h. J Med Chem. 2020 Jan 23;63(2):512-528. doi: 10.1021/acs.jmedchem.9b01293. Epub 2019 Nov 27. J Med Chem. 2020. PMID: 31721572
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.
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
SAR439859, a Novel Selective Estrogen Receptor Degrader (SERD), Demonstrates Effective and Broad Antitumor Activity in Wild-Type and Mutant ER-Positive Breast Cancer Models.
Shomali M, Cheng J, Sun F, Koundinya M, Guo Z, Hebert AT, McManus J, Levit MN, Hoffmann D, Courjaud A, Arrebola R, Cao H, Pollard J, Lee JS, Besret L, Caron A, Bangari DS, Abecassis PY, Schio L, El-Ahmad Y, Halley F, Tabart M, Certal V, Thompson F, McCort G, Filoche-Rommé B, Cheng H, Garcia-Echeverria C, Debussche L, Bouaboula M. Shomali M, et al. Among authors: cheng j, cheng h. Mol Cancer Ther. 2021 Feb;20(2):250-262. doi: 10.1158/1535-7163.MCT-20-0390. Epub 2020 Dec 11. Mol Cancer Ther. 2021. PMID: 33310762
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
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