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Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer.
LaMarche MJ, Acker M, Argintaru A, Bauer D, Boisclair J, Chan H, Chen CH, Chen YN, Chen Z, Deng Z, Dore M, Dunstan D, Fan J, Fekkes P, Firestone B, Fodor M, Garcia-Fortanet J, Fortin PD, Fridrich C, Giraldes J, Glick M, Grunenfelder D, Hao HX, Hentemann M, Ho S, Jouk A, Kang ZB, Karki R, Kato M, Keen N, Koenig R, LaBonte LR, Larrow J, Liu G, Liu S, Majumdar D, Mathieu S, Meyer MJ, Mohseni M, Ntaganda R, Palermo M, Perez L, Pu M, Ramsey T, Reilly J, Sarver P, Sellers WR, Sendzik M, Shultz MD, Slisz J, Slocum K, Smith T, Spence S, Stams T, Straub C, Tamez V Jr, Toure BB, Towler C, Wang P, Wang H, Williams SL, Yang F, Yu B, Zhang JH, Zhu S. LaMarche MJ, et al. Among authors: meyer mj. J Med Chem. 2020 Nov 25;63(22):13578-13594. doi: 10.1021/acs.jmedchem.0c01170. Epub 2020 Sep 24. J Med Chem. 2020. PMID: 32910655
Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor.
Garcia Fortanet J, Chen CH, Chen YN, Chen Z, Deng Z, Firestone B, Fekkes P, Fodor M, Fortin PD, Fridrich C, Grunenfelder D, Ho S, Kang ZB, Karki R, Kato M, Keen N, LaBonte LR, Larrow J, Lenoir F, Liu G, Liu S, Lombardo F, Majumdar D, Meyer MJ, Palermo M, Perez L, Pu M, Ramsey T, Sellers WR, Shultz MD, Stams T, Towler C, Wang P, Williams SL, Zhang JH, LaMarche MJ. Garcia Fortanet J, et al. Among authors: meyer mj. J Med Chem. 2016 Sep 8;59(17):7773-82. doi: 10.1021/acs.jmedchem.6b00680. Epub 2016 Jul 12. J Med Chem. 2016. PMID: 27347692
Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases.
Chen YN, LaMarche MJ, Chan HM, Fekkes P, Garcia-Fortanet J, Acker MG, Antonakos B, Chen CH, Chen Z, Cooke VG, Dobson JR, Deng Z, Fei F, Firestone B, Fodor M, Fridrich C, Gao H, Grunenfelder D, Hao HX, Jacob J, Ho S, Hsiao K, Kang ZB, Karki R, Kato M, Larrow J, La Bonte LR, Lenoir F, Liu G, Liu S, Majumdar D, Meyer MJ, Palermo M, Perez L, Pu M, Price E, Quinn C, Shakya S, Shultz MD, Slisz J, Venkatesan K, Wang P, Warmuth M, Williams S, Yang G, Yuan J, Zhang JH, Zhu P, Ramsey T, Keen NJ, Sellers WR, Stams T, Fortin PD. Chen YN, et al. Among authors: meyer mj. Nature. 2016 Jul 7;535(7610):148-52. doi: 10.1038/nature18621. Epub 2016 Jun 29. Nature. 2016. PMID: 27362227
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: meyer mj. 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
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: meyer mj. 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
Discovery and Optimization of HKT288, a Cadherin-6-Targeting ADC for the Treatment of Ovarian and Renal Cancers.
Bialucha CU, Collins SD, Li X, Saxena P, Zhang X, Dürr C, Lafont B, Prieur P, Shim Y, Mosher R, Lee D, Ostrom L, Hu T, Bilic S, Rajlic IL, Capka V, Jiang W, Wagner JP, Elliott G, Veloso A, Piel JC, Flaherty MM, Mansfield KG, Meseck EK, Rubic-Schneider T, London AS, Tschantz WR, Kurz M, Nguyen D, Bourret A, Meyer MJ, Faris JE, Janatpour MJ, Chan VW, Yoder NC, Catcott KC, McShea MA, Sun X, Gao H, Williams J, Hofmann F, Engelman JA, Ettenberg SA, Sellers WR, Lees E. Bialucha CU, et al. Among authors: meyer mj. Cancer Discov. 2017 Sep;7(9):1030-1045. doi: 10.1158/2159-8290.CD-16-1414. Epub 2017 May 19. Cancer Discov. 2017. PMID: 28526733
New Imidazodiazepine Analogue, 5-(8-Bromo-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepin-3-yl)oxazole, Provides a Simplified Synthetic Scheme, High Oral Plasma and Brain Exposures, and Produces Antiseizure Efficacy in Mice, and Antiepileptogenic Activity in Neural Networks in Brain Slices from a Patient with Mesial Temporal Lobe Epilepsy.
Sharmin D, Divović B, Ping X, Cerne R, Smith JL, Rezvanian S, Mondal P, Meyer MJ, Kiley ME, Arnold LA, Mian MY, Pandey KP, Jin X, Mitrović JR, Djorović D, Lippa A, Cook JM, Golani LK, Scholze P, Savić MM, Witkin JM. Sharmin D, et al. Among authors: meyer mj. ACS Chem Neurosci. 2024 Feb 7;15(3):517-526. doi: 10.1021/acschemneuro.3c00555. Epub 2024 Jan 4. ACS Chem Neurosci. 2024. PMID: 38175916
173 results