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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: lamarche mj. 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
Discovery of Darovasertib (NVP-LXS196), a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma.
Visser M, Papillon JPN, Luzzio M, LaMarche MJ, Fan J, Michael W, Wang D, Zhang A, Straub C, Mathieu S, Kato M, Palermo M, Chen C, Ramsey T, Joud C, Barrett R, Vattay A, Guo R, Bric A, Chung F, Liang G, Romanowski MJ, Lam J, Thohan S, Atassi F, Wylie A, Cooke VG. Visser M, et al. Among authors: lamarche mj. J Med Chem. 2024 Jan 25;67(2):1447-1459. doi: 10.1021/acs.jmedchem.3c02002. Epub 2024 Jan 10. J Med Chem. 2024. PMID: 38198520
Think Biologically, Act Chemically.
LaMarche MJ. LaMarche MJ. J Med Chem. 2022 Sep 8;65(17):11478-11484. doi: 10.1021/acs.jmedchem.2c01121. Epub 2022 Aug 18. J Med Chem. 2022. PMID: 35981217 Review.
SHP2 blockade enhances anti-tumor immunity via tumor cell intrinsic and extrinsic mechanisms.
Wang Y, Mohseni M, Grauel A, Diez JE, Guan W, Liang S, Choi JE, Pu M, Chen D, Laszewski T, Schwartz S, Gu J, Mansur L, Burks T, Brodeur L, Velazquez R, Kovats S, Pant B, Buruzula G, Deng E, Chen JT, Sari-Sarraf F, Dornelas C, Varadarajan M, Yu H, Liu C, Lim J, Hao HX, Jiang X, Malamas A, LaMarche MJ, Geyer FC, McLaughlin M, Costa C, Wagner J, Ruddy D, Jayaraman P, Kirkpatrick ND, Zhang P, Iartchouk O, Aardalen K, Cremasco V, Dranoff G, Engelman JA, Silver S, Wang H, Hastings WD, Goldoni S. Wang Y, et al. Among authors: lamarche mj. Sci Rep. 2021 Jan 14;11(1):1399. doi: 10.1038/s41598-021-80999-x. Sci Rep. 2021. PMID: 33446805 Free PMC article.
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: lamarche 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
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. 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
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: lamarche 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
42 results