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Page 1
c-Met inhibitors with novel binding mode show activity against several hereditary papillary renal cell carcinoma-related mutations.
Bellon SF, Kaplan-Lefko P, Yang Y, Zhang Y, Moriguchi J, Rex K, Johnson CW, Rose PE, Long AM, O'Connor AB, Gu Y, Coxon A, Kim TS, Tasker A, Burgess TL, Dussault I. Bellon SF, et al. Among authors: dussault i. J Biol Chem. 2008 Feb 1;283(5):2675-83. doi: 10.1074/jbc.M705774200. Epub 2007 Nov 30. J Biol Chem. 2008. PMID: 18055465 Free article.
Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.
Albrecht BK, Harmange JC, Bauer D, Berry L, Bode C, Boezio AA, Chen A, Choquette D, Dussault I, Fridrich C, Hirai S, Hoffman D, Larrow JF, Kaplan-Lefko P, Lin J, Lohman J, Long AM, Moriguchi J, O'Connor A, Potashman MH, Reese M, Rex K, Siegmund A, Shah K, Shimanovich R, Springer SK, Teffera Y, Yang Y, Zhang Y, Bellon SF. Albrecht BK, et al. Among authors: dussault i. J Med Chem. 2008 May 22;51(10):2879-82. doi: 10.1021/jm800043g. Epub 2008 Apr 22. J Med Chem. 2008. PMID: 18426196
Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).
Liu L, Siegmund A, Xi N, Kaplan-Lefko P, Rex K, Chen A, Lin J, Moriguchi J, Berry L, Huang L, Teffera Y, Yang Y, Zhang Y, Bellon SF, Lee M, Shimanovich R, Bak A, Dominguez C, Norman MH, Harmange JC, Dussault I, Kim TS. Liu L, et al. Among authors: dussault i. J Med Chem. 2008 Jul 10;51(13):3688-91. doi: 10.1021/jm800401t. Epub 2008 Jun 14. J Med Chem. 2008. PMID: 18553959
Design, synthesis, and biological evaluation of potent c-Met inhibitors.
D'Angelo ND, Bellon SF, Booker SK, Cheng Y, Coxon A, Dominguez C, Fellows I, Hoffman D, Hungate R, Kaplan-Lefko P, Lee MR, Li C, Liu L, Rainbeau E, Reider PJ, Rex K, Siegmund A, Sun Y, Tasker AS, Xi N, Xu S, Yang Y, Zhang Y, Burgess TL, Dussault I, Kim TS. D'Angelo ND, et al. Among authors: dussault i. J Med Chem. 2008 Sep 25;51(18):5766-79. doi: 10.1021/jm8006189. J Med Chem. 2008. PMID: 18763753
In Vitro and In Vivo Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models.
Hughes PE, Rex K, Caenepeel S, Yang Y, Zhang Y, Broome MA, Kha HT, Burgess TL, Amore B, Kaplan-Lefko PJ, Moriguchi J, Werner J, Damore MA, Baker D, Choquette DM, Harmange JC, Radinsky R, Kendall R, Dussault I, Coxon A. Hughes PE, et al. Among authors: dussault i. Mol Cancer Ther. 2016 Jul;15(7):1568-79. doi: 10.1158/1535-7163.MCT-15-0871. Epub 2016 Apr 19. Mol Cancer Ther. 2016. PMID: 27196782
Selective MET Kinase Inhibition in MET-Dependent Glioma Models Alters Gene Expression and Induces Tumor Plasticity.
van den Heuvel CNAM, Navis AC, de Bitter T, Amiri H, Verrijp K, Heerschap A, Rex K, Dussault I, Caenepeel S, Coxon A, Span PN, Wesseling P, Hendriks W, Leenders WPJ. van den Heuvel CNAM, et al. Among authors: dussault i. Mol Cancer Res. 2017 Nov;15(11):1587-1597. doi: 10.1158/1541-7786.MCR-17-0177. Epub 2017 Jul 27. Mol Cancer Res. 2017. PMID: 28751462
Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors.
Boezio AA, Berry L, Albrecht BK, Bauer D, Bellon SF, Bode C, Chen A, Choquette D, Dussault I, Fang M, Hirai S, Kaplan-Lefko P, Larrow JF, Lin MH, Lohman J, Potashman MH, Qu Y, Rex K, Santostefano M, Shah K, Shimanovich R, Springer SK, Teffera Y, Yang Y, Zhang Y, Harmange JC. Boezio AA, et al. Among authors: dussault i. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6307-12. doi: 10.1016/j.bmcl.2009.09.096. Epub 2009 Sep 27. Bioorg Med Chem Lett. 2009. PMID: 19819693
STK33 kinase activity is nonessential in KRAS-dependent cancer cells.
Babij C, Zhang Y, Kurzeja RJ, Munzli A, Shehabeldin A, Fernando M, Quon K, Kassner PD, Ruefli-Brasse AA, Watson VJ, Fajardo F, Jackson A, Zondlo J, Sun Y, Ellison AR, Plewa CA, San MT, Robinson J, McCarter J, Schwandner R, Judd T, Carnahan J, Dussault I. Babij C, et al. Among authors: dussault i. Cancer Res. 2011 Sep 1;71(17):5818-26. doi: 10.1158/0008-5472.CAN-11-0778. Epub 2011 Jul 8. Cancer Res. 2011. PMID: 21742770
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.
Liu L, Norman MH, Lee M, Xi N, Siegmund A, Boezio AA, Booker S, Choquette D, D'Angelo ND, Germain J, Yang K, Yang Y, Zhang Y, Bellon SF, Whittington DA, Harmange JC, Dominguez C, Kim TS, Dussault I. Liu L, et al. Among authors: dussault i. J Med Chem. 2012 Mar 8;55(5):1868-97. doi: 10.1021/jm201331s. Epub 2012 Feb 24. J Med Chem. 2012. PMID: 22320327
49 results