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Page 1
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: moriguchi j. J Med Chem. 2008 Jul 10;51(13):3688-91. doi: 10.1021/jm800401t. Epub 2008 Jun 14. J Med Chem. 2008. PMID: 18553959
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: moriguchi j. 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: moriguchi j. J Med Chem. 2008 May 22;51(10):2879-82. doi: 10.1021/jm800043g. Epub 2008 Apr 22. J Med Chem. 2008. PMID: 18426196
Conatumumab, a fully human agonist antibody to death receptor 5, induces apoptosis via caspase activation in multiple tumor types.
Kaplan-Lefko PJ, Graves JD, Zoog SJ, Pan Y, Wall J, Branstetter DG, Moriguchi J, Coxon A, Huard JN, Xu R, Peach ML, Juan G, Kaufman S, Chen Q, Bianchi A, Kordich JJ, Ma M, Foltz IN, Gliniak BC. Kaplan-Lefko PJ, et al. Among authors: moriguchi j. Cancer Biol Ther. 2010 Apr 15;9(8):618-31. doi: 10.4161/cbt.9.8.11264. Epub 2010 Apr 20. Cancer Biol Ther. 2010. PMID: 20150762 Free article.
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: moriguchi j. 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
Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe.
Tamayo NA, Bourbeau MP, Allen JR, Ashton KS, Chen JJ, Kaller MR, Nguyen TT, Nishimura N, Pettus LH, Walton M, Belmontes B, Moriguchi J, Chen K, McCarter JD, Hanestad K, Chung G, Ninniri MSS, Sun J, Poppe L, Spahr C, Hui J, Jia L, Wu T, Dahal UP, Edson KZ, Payton M. Tamayo NA, et al. Among authors: moriguchi j. J Med Chem. 2022 Mar 24;65(6):4972-4990. doi: 10.1021/acs.jmedchem.1c02030. Epub 2022 Mar 14. J Med Chem. 2022. PMID: 35286090
AMG 193, a Clinical Stage MTA-Cooperative PRMT5 Inhibitor, Drives Antitumor Activity Preclinically and in Patients With MTAP-Deleted Cancers.
Belmontes B, Slemmons KK, Su C, Liu S, Policheni AN, Moriguchi J, Tan H, Xie F, Aiello DA, Yang Y, Lazaro R, Aeffner F, Rees MG, Ronan MM, Roth JA, Vestergaard M, Cowland S, Andersson J, Sarvary I, Chen Q, Sharma P, Lopez P, Tamayo N, Pettus LH, Ghimire-Rijal S, Mukund S, Allen JR, DeVoss J, Coxon A, Rodon J, Ghiringhelli F, Penel N, Prenen H, Glad S, Chuang CH, Keyvanjah K, Townsley DM, Butler JR, Bourbeau MP, Caenepeel S, Hughes PE. Belmontes B, et al. Among authors: moriguchi j. Cancer Discov. 2024 Sep 16. doi: 10.1158/2159-8290.CD-24-0887. Online ahead of print. Cancer Discov. 2024. PMID: 39282709
215 results