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14,750 results

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Page 1
Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist.
Pan S, Wu X, Jiang J, Gao W, Wan Y, Cheng D, Han D, Liu J, Englund NP, Wang Y, Peukert S, Miller-Moslin K, Yuan J, Guo R, Matsumoto M, Vattay A, Jiang Y, Tsao J, Sun F, Pferdekamper AC, Dodd S, Tuntland T, Maniara W, Kelleher JF 3rd, Yao YM, Warmuth M, Williams J, Dorsch M. Pan S, et al. Among authors: yuan j. ACS Med Chem Lett. 2010 Mar 16;1(3):130-4. doi: 10.1021/ml1000307. eCollection 2010 Jun 10. ACS Med Chem Lett. 2010. PMID: 24900187 Free PMC article.
1-amino-4-benzylphthalazines as orally bioavailable smoothened antagonists with antitumor activity.
Miller-Moslin K, Peukert S, Jain RK, McEwan MA, Karki R, Llamas L, Yusuff N, He F, Li Y, Sun Y, Dai M, Perez L, Michael W, Sheng T, Lei H, Zhang R, Williams J, Bourret A, Ramamurthy A, Yuan J, Guo R, Matsumoto M, Vattay A, Maniara W, Amaral A, Dorsch M, Kelleher JF 3rd. Miller-Moslin K, et al. Among authors: yuan j. J Med Chem. 2009 Jul 9;52(13):3954-68. doi: 10.1021/jm900309j. J Med Chem. 2009. PMID: 19469545
Interfering with resistance to smoothened antagonists by inhibition of the PI3K pathway in medulloblastoma.
Buonamici S, Williams J, Morrissey M, Wang A, Guo R, Vattay A, Hsiao K, Yuan J, Green J, Ospina B, Yu Q, Ostrom L, Fordjour P, Anderson DL, Monahan JE, Kelleher JF, Peukert S, Pan S, Wu X, Maira SM, García-Echeverría C, Briggs KJ, Watkins DN, Yao YM, Lengauer C, Warmuth M, Sellers WR, Dorsch M. Buonamici S, et al. Among authors: yuan j. Sci Transl Med. 2010 Sep 29;2(51):51ra70. doi: 10.1126/scitranslmed.3001599. Sci Transl Med. 2010. PMID: 20881279 Free PMC article.
Discovery of NVP-LEQ506, a second-generation inhibitor of smoothened.
Peukert S, He F, Dai M, Zhang R, Sun Y, Miller-Moslin K, McEwan M, Lagu B, Wang K, Yusuff N, Bourret A, Ramamurthy A, Maniara W, Amaral A, Vattay A, Wang A, Guo R, Yuan J, Green J, Williams J, Buonamici S, Kelleher JF 3rd, Dorsch M. Peukert S, et al. Among authors: yuan j. ChemMedChem. 2013 Aug;8(8):1261-5. doi: 10.1002/cmdc.201300217. Epub 2013 Jul 2. ChemMedChem. 2013. PMID: 23821351 No abstract available.
Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic.
Ramurthy S, Taft BR, Aversa RJ, Barsanti PA, Burger MT, Lou Y, Nishiguchi GA, Rico A, Setti L, Smith A, Subramanian S, Tamez V, Tanner H, Wan L, Hu C, Appleton BA, Mamo M, Tandeske L, Tellew JE, Huang S, Yue Q, Chaudhary A, Tian H, Iyer R, Hassan AQ, Mathews Griner LA, La Bonte LR, Cooke VG, Van Abbema A, Merritt H, Gampa K, Feng F, Yuan J, Mishina Y, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Sellers WR, Lees E, Shao W, Dillon MP, Stuart DD. Ramurthy S, et al. Among authors: yuan j. J Med Chem. 2020 Mar 12;63(5):2013-2027. doi: 10.1021/acs.jmedchem.9b00161. Epub 2019 May 16. J Med Chem. 2020. PMID: 31059256
Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.
Nishiguchi GA, Rico A, Tanner H, Aversa RJ, Taft BR, Subramanian S, Setti L, Burger MT, Wan L, Tamez V, Smith A, Lou Y, Barsanti PA, Appleton BA, Mamo M, Tandeske L, Dix I, Tellew JE, Huang S, Mathews Griner LA, Cooke VG, Van Abbema A, Merritt H, Ma S, Gampa K, Feng F, Yuan J, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Jansen JM, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Lees E, Shao W, Stuart DD, Dillon MP, Ramurthy S. Nishiguchi GA, et al. Among authors: yuan j. J Med Chem. 2017 Jun 22;60(12):4869-4881. doi: 10.1021/acs.jmedchem.6b01862. Epub 2017 Jun 8. J Med Chem. 2017. PMID: 28557458
A crucial requirement for Hedgehog signaling in small cell lung cancer.
Park KS, Martelotto LG, Peifer M, Sos ML, Karnezis AN, Mahjoub MR, Bernard K, Conklin JF, Szczepny A, Yuan J, Guo R, Ospina B, Falzon J, Bennett S, Brown TJ, Markovic A, Devereux WL, Ocasio CA, Chen JK, Stearns T, Thomas RK, Dorsch M, Buonamici S, Watkins DN, Peacock CD, Sage J. Park KS, et al. Among authors: yuan j. Nat Med. 2011 Oct 9;17(11):1504-8. doi: 10.1038/nm.2473. Nat Med. 2011. PMID: 21983857 Free PMC article.
Inhibition of tumorigenesis driven by different Wnt proteins requires blockade of distinct ligand-binding regions by LRP6 antibodies.
Ettenberg SA, Charlat O, Daley MP, Liu S, Vincent KJ, Stuart DD, Schuller AG, Yuan J, Ospina B, Green J, Yu Q, Walsh R, Li S, Schmitz R, Heine H, Bilic S, Ostrom L, Mosher R, Hartlepp KF, Zhu Z, Fawell S, Yao YM, Stover D, Finan PM, Porter JA, Sellers WR, Klagge IM, Cong F. Ettenberg SA, et al. Among authors: yuan j. Proc Natl Acad Sci U S A. 2010 Aug 31;107(35):15473-8. doi: 10.1073/pnas.1007428107. Epub 2010 Aug 16. Proc Natl Acad Sci U S A. 2010. PMID: 20713706 Free PMC article.
LXH254, a Potent and Selective ARAF-Sparing Inhibitor of BRAF and CRAF for the Treatment of MAPK-Driven Tumors.
Monaco KA, Delach S, Yuan J, Mishina Y, Fordjour P, Labrot E, McKay D, Guo R, Higgins S, Wang HQ, Liang J, Bui K, Green J, Aspesi P, Ambrose J, Mapa F, Griner L, Jaskelioff M, Fuller J, Crawford K, Pardee G, Widger S, Hammerman PS, Engelman JA, Stuart DD, Cooke VG, Caponigro G. Monaco KA, et al. Among authors: yuan j. Clin Cancer Res. 2021 Apr 1;27(7):2061-2073. doi: 10.1158/1078-0432.CCR-20-2563. Epub 2020 Dec 22. Clin Cancer Res. 2021. PMID: 33355204
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