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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: wang p. Nature. 2016 Jul 7;535(7610):148-52. doi: 10.1038/nature18621. Epub 2016 Jun 29. Nature. 2016. PMID: 27362227
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: wang p. 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
Dual Allosteric Inhibition of SHP2 Phosphatase.
Fodor M, Price E, Wang P, Lu H, Argintaru A, Chen Z, Glick M, Hao HX, Kato M, Koenig R, LaRochelle JR, Liu G, McNeill E, Majumdar D, Nishiguchi GA, Perez LB, Paris G, Quinn CM, Ramsey T, Sendzik M, Shultz MD, Williams SL, Stams T, Blacklow SC, Acker MG, LaMarche MJ. Fodor M, et al. Among authors: wang p. ACS Chem Biol. 2018 Mar 16;13(3):647-656. doi: 10.1021/acschembio.7b00980. Epub 2018 Jan 18. ACS Chem Biol. 2018. PMID: 29304282
Optimization of Fused Bicyclic Allosteric SHP2 Inhibitors.
Bagdanoff JT, Chen Z, Acker M, Chen YN, Chan H, Dore M, Firestone B, Fodor M, Fortanet J, Hentemann M, Kato M, Koenig R, LaBonte LR, Liu S, Mohseni M, Ntaganda R, Sarver P, Smith T, Sendzik M, Stams T, Spence S, Towler C, Wang H, Wang P, Williams SL, LaMarche MJ. Bagdanoff JT, et al. Among authors: wang h, wang p. J Med Chem. 2019 Feb 28;62(4):1781-1792. doi: 10.1021/acs.jmedchem.8b01725. Epub 2019 Feb 8. J Med Chem. 2019. PMID: 30688462
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: wang h, wang p. 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
6-Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors.
Sarver P, Acker M, Bagdanoff JT, Chen Z, Chen YN, Chan H, Firestone B, Fodor M, Fortanet J, Hao H, Hentemann M, Kato M, Koenig R, LaBonte LR, Liu G, Liu S, Liu C, McNeill E, Mohseni M, Sendzik M, Stams T, Spence S, Tamez V, Tichkule R, Towler C, Wang H, Wang P, Williams SL, Yu B, LaMarche MJ. Sarver P, et al. Among authors: wang h, wang p. J Med Chem. 2019 Feb 28;62(4):1793-1802. doi: 10.1021/acs.jmedchem.8b01726. Epub 2019 Feb 16. J Med Chem. 2019. PMID: 30688459
Correction to Optimization of Fused Bicyclic Allosteric SHP2 Inhibitors.
Bagdanoff JT, Chen Z, Acker M, Chen YN, Chan H, Dore M, Firestone B, Fodor M, Fortanet J, Hentemann M, Kato M, Koenig R, LaBonte LR, Liu S, Mohseni M, Ntaganda R, Sarver P, Shultz MD, Smith T, Sendzik M, Stams T, Spence S, Towler C, Wang H, Wang P, Williams SL, LaMarche MJ. Bagdanoff JT, et al. Among authors: wang h, wang p. J Med Chem. 2019 Apr 11;62(7):3780. doi: 10.1021/acs.jmedchem.9b00435. Epub 2019 Mar 22. J Med Chem. 2019. PMID: 30900881 No abstract available.
Correction to 6-Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors.
Sarver P, Acker M, Bagdanoff JT, Chen Z, Chen YN, Chan H, Firestone B, Fodor M, Fortanet J, Hao H, Hentemann M, Jouk A, Kato M, Koenig R, LaBonte LR, Liu G, Liu S, Liu C, McNeill E, Mohseni M, Shultz MD, Sendzik M, Stams T, Spence S, Tamez V, Tichkule R, Towler C, Wang H, Wang P, Williams SL, Yu B, LaMarche MJ. Sarver P, et al. Among authors: wang h, wang p. J Med Chem. 2019 Apr 11;62(7):3781. doi: 10.1021/acs.jmedchem.9b00436. Epub 2019 Mar 22. J Med Chem. 2019. PMID: 30900883 No abstract available.
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