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Page 1
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.
Gould AE, Adams R, Adhikari S, Aertgeerts K, Afroze R, Blackburn C, Calderwood EF, Chau R, Chouitar J, Duffey MO, England DB, Farrer C, Forsyth N, Garcia K, Gaulin J, Greenspan PD, Guo R, Harrison SJ, Huang SC, Iartchouk N, Janowick D, Kim MS, Kulkarni B, Langston SP, Liu JX, Ma LT, Menon S, Mizutani H, Paske E, Renou CC, Rezaei M, Rowland RS, Sintchak MD, Smith MD, Stroud SG, Tregay M, Tian Y, Veiby OP, Vos TJ, Vyskocil S, Williams J, Xu T, Yang JJ, Yano J, Zeng H, Zhang DM, Zhang Q, Galvin KM. Gould AE, et al. Among authors: williams j. J Med Chem. 2011 Mar 24;54(6):1836-46. doi: 10.1021/jm101479y. Epub 2011 Feb 22. J Med Chem. 2011. PMID: 21341678
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: williams j. J Med Chem. 2009 Jul 9;52(13):3954-68. doi: 10.1021/jm900309j. J Med Chem. 2009. PMID: 19469545
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: williams 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.
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: williams j. ChemMedChem. 2013 Aug;8(8):1261-5. doi: 10.1002/cmdc.201300217. Epub 2013 Jul 2. ChemMedChem. 2013. PMID: 23821351 No abstract available.
Tumor Intrinsic Efficacy by SHP2 and RTK Inhibitors in KRAS-Mutant Cancers.
Hao HX, Wang H, Liu C, Kovats S, Velazquez R, Lu H, Pant B, Shirley M, Meyer MJ, Pu M, Lim J, Fleming M, Alexander L, Farsidjani A, LaMarche MJ, Moody S, Silver SJ, Caponigro G, Stuart DD, Abrams TJ, Hammerman PS, Williams J, Engelman JA, Goldoni S, Mohseni M. Hao HX, et al. Among authors: williams j. Mol Cancer Ther. 2019 Dec;18(12):2368-2380. doi: 10.1158/1535-7163.MCT-19-0170. Epub 2019 Aug 22. Mol Cancer Ther. 2019. PMID: 31439712
Combinations with Allosteric SHP2 Inhibitor TNO155 to Block Receptor Tyrosine Kinase Signaling.
Liu C, Lu H, Wang H, Loo A, Zhang X, Yang G, Kowal C, Delach S, Wang Y, Goldoni S, Hastings WD, Wong K, Gao H, Meyer MJ, Moody SE, LaMarche MJ, Engelman JA, Williams JA, Hammerman PS, Abrams TJ, Mohseni M, Caponigro G, Hao HX. Liu C, et al. Among authors: williams ja. Clin Cancer Res. 2021 Jan 1;27(1):342-354. doi: 10.1158/1078-0432.CCR-20-2718. Epub 2020 Oct 12. Clin Cancer Res. 2021. PMID: 33046519
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: williams j. Sci Transl Med. 2010 Sep 29;2(51):51ra70. doi: 10.1126/scitranslmed.3001599. Sci Transl Med. 2010. PMID: 20881279 Free PMC article.
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