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Page 1
Exploiting MCL1 Dependency with Combination MEK + MCL1 Inhibitors Leads to Induction of Apoptosis and Tumor Regression in KRAS-Mutant Non-Small Cell Lung Cancer.
Nangia V, Siddiqui FM, Caenepeel S, Timonina D, Bilton SJ, Phan N, Gomez-Caraballo M, Archibald HL, Li C, Fraser C, Rigas D, Vajda K, Ferris LA, Lanuti M, Wright CD, Raskin KA, Cahill DP, Shin JH, Keyes C, Sequist LV, Piotrowska Z, Farago AF, Azzoli CG, Gainor JF, Sarosiek KA, Brown SP, Coxon A, Benes CH, Hughes PE, Hata AN. Nangia V, et al. Among authors: hughes pe. Cancer Discov. 2018 Dec;8(12):1598-1613. doi: 10.1158/2159-8290.CD-18-0277. Epub 2018 Sep 25. Cancer Discov. 2018. PMID: 30254092 Free PMC article.
Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor.
Hodous BL, Geuns-Meyer SD, Hughes PE, Albrecht BK, Bellon S, Bready J, Caenepeel S, Cee VJ, Chaffee SC, Coxon A, Emery M, Fretland J, Gallant P, Gu Y, Hoffman D, Johnson RE, Kendall R, Kim JL, Long AM, Morrison M, Olivieri PR, Patel VF, Polverino A, Rose P, Tempest P, Wang L, Whittington DA, Zhao H. Hodous BL, et al. Among authors: hughes pe. J Med Chem. 2007 Feb 22;50(4):611-26. doi: 10.1021/jm061107l. Epub 2007 Jan 25. J Med Chem. 2007. PMID: 17253678
Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase.
Cee VJ, Albrecht BK, Geuns-Meyer S, Hughes P, Bellon S, Bready J, Caenepeel S, Chaffee SC, Coxon A, Emery M, Fretland J, Gallant P, Gu Y, Hodous BL, Hoffman D, Johnson RE, Kendall R, Kim JL, Long AM, McGowan D, Morrison M, Olivieri PR, Patel VF, Polverino A, Powers D, Rose P, Wang L, Zhao H. Cee VJ, et al. J Med Chem. 2007 Feb 22;50(4):627-40. doi: 10.1021/jm061112p. Epub 2007 Jan 25. J Med Chem. 2007. PMID: 17253679
Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.
Cee VJ, Cheng AC, Romero K, Bellon S, Mohr C, Whittington DA, Bak A, Bready J, Caenepeel S, Coxon A, Deak HL, Fretland J, Gu Y, Hodous BL, Huang X, Kim JL, Lin J, Long AM, Nguyen H, Olivieri PR, Patel VF, Wang L, Zhou Y, Hughes P, Geuns-Meyer S. Cee VJ, et al. Bioorg Med Chem Lett. 2009 Jan 15;19(2):424-7. doi: 10.1016/j.bmcl.2008.11.056. Epub 2008 Nov 20. Bioorg Med Chem Lett. 2009. PMID: 19062275
Broad antitumor activity in breast cancer xenografts by motesanib, a highly selective, oral inhibitor of vascular endothelial growth factor, platelet-derived growth factor, and Kit receptors.
Coxon A, Bush T, Saffran D, Kaufman S, Belmontes B, Rex K, Hughes P, Caenepeel S, Rottman JB, Tasker A, Patel V, Kendall R, Radinsky R, Polverino A. Coxon A, et al. Clin Cancer Res. 2009 Jan 1;15(1):110-8. doi: 10.1158/1078-0432.CCR-08-1155. Clin Cancer Res. 2009. PMID: 19118038
Motesanib inhibits Kit mutations associated with gastrointestinal stromal tumors.
Caenepeel S, Renshaw-Gegg L, Baher A, Bush TL, Baron W, Juan T, Manoukian R, Tasker AS, Polverino A, Hughes PE. Caenepeel S, et al. Among authors: hughes pe. J Exp Clin Cancer Res. 2010 Jul 15;29(1):96. doi: 10.1186/1756-9966-29-96. J Exp Clin Cancer Res. 2010. PMID: 20633291 Free PMC article.
Context-dependent role of angiopoietin-1 inhibition in the suppression of angiogenesis and tumor growth: implications for AMG 386, an angiopoietin-1/2-neutralizing peptibody.
Coxon A, Bready J, Min H, Kaufman S, Leal J, Yu D, Lee TA, Sun JR, Estrada J, Bolon B, McCabe J, Wang L, Rex K, Caenepeel S, Hughes P, Cordover D, Kim H, Han SJ, Michaels ML, Hsu E, Shimamoto G, Cattley R, Hurh E, Nguyen L, Wang SX, Ndifor A, Hayward IJ, Falcón BL, McDonald DM, Li L, Boone T, Kendall R, Radinsky R, Oliner JD. Coxon A, et al. Mol Cancer Ther. 2010 Oct;9(10):2641-51. doi: 10.1158/1535-7163.MCT-10-0213. Mol Cancer Ther. 2010. PMID: 20937592 Free PMC article.
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.
D'Angelo ND, Kim TS, Andrews K, Booker SK, Caenepeel S, Chen K, D'Amico D, Freeman D, Jiang J, Liu L, McCarter JD, San Miguel T, Mullady EL, Schrag M, Subramanian R, Tang J, Wahl RC, Wang L, Whittington DA, Wu T, Xi N, Xu Y, Yakowec P, Yang K, Zalameda LP, Zhang N, Hughes P, Norman MH. D'Angelo ND, et al. J Med Chem. 2011 Mar 24;54(6):1789-811. doi: 10.1021/jm1014605. Epub 2011 Feb 18. J Med Chem. 2011. PMID: 21332118
Anti-tumor activity of motesanib in a medullary thyroid cancer model.
Coxon A, Bready J, Kaufman S, Estrada J, Osgood T, Canon J, Wang L, Radinsky R, Kendall R, Hughes P, Polverino A. Coxon A, et al. J Endocrinol Invest. 2012 Feb;35(2):181-90. doi: 10.3275/7609. Epub 2011 Mar 21. J Endocrinol Invest. 2012. PMID: 21422803
Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.
Nishimura N, Siegmund A, Liu L, Yang K, Bryan MC, Andrews KL, Bo Y, Booker SK, Caenepeel S, Freeman D, Liao H, McCarter J, Mullady EL, San Miguel T, Subramanian R, Tamayo N, Wang L, Whittington DA, Zalameda L, Zhang N, Hughes PE, Norman MH. Nishimura N, et al. Among authors: hughes pe. J Med Chem. 2011 Jul 14;54(13):4735-51. doi: 10.1021/jm200386s. Epub 2011 Jun 20. J Med Chem. 2011. PMID: 21612232
134 results