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Page 1
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: fridrich c. 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: fridrich c. 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
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: fridrich c. 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
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: fridrich c. 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 Small Molecule Splicing Modulators of Survival Motor Neuron-2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA).
Cheung AK, Hurley B, Kerrigan R, Shu L, Chin DN, Shen Y, O'Brien G, Sung MJ, Hou Y, Axford J, Cody E, Sun R, Fazal A, Fridrich C, Sanchez CC, Tomlinson RC, Jain M, Deng L, Hoffmaster K, Song C, Van Hoosear M, Shin Y, Servais R, Towler C, Hild M, Curtis D, Dietrich WF, Hamann LG, Briner K, Chen KS, Kobayashi D, Sivasankaran R, Dales NA. Cheung AK, et al. Among authors: fridrich c. J Med Chem. 2018 Dec 27;61(24):11021-11036. doi: 10.1021/acs.jmedchem.8b01291. Epub 2018 Dec 13. J Med Chem. 2018. PMID: 30407821
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.
Lorthiois E, Roache J, Barnes-Seeman D, Altmann E, Hassiepen U, Turner G, Duvadie R, Hornak V, Karki RG, Schiering N, Weihofen WA, Perruccio F, Calhoun A, Fazal T, Dedic D, Durand C, Dussauge S, Fettis K, Tritsch F, Dentel C, Druet A, Liu D, Kirman L, Lachal J, Namoto K, Bevan D, Mo R, Monnet G, Muller L, Zessis R, Huang X, Lindsley L, Currie T, Chiu YH, Fridrich C, Delgado P, Wang S, Hollis-Symynkywicz M, Berghausen J, Williams E, Liu H, Liang G, Kim H, Hoffmann P, Hein A, Ramage P, D'Arcy A, Harlfinger S, Renatus M, Ruedisser S, Feldman D, Elliott J, Sedrani R, Maibaum J, Adams CM. Lorthiois E, et al. Among authors: fridrich c. J Med Chem. 2020 Aug 13;63(15):8088-8113. doi: 10.1021/acs.jmedchem.0c00279. Epub 2020 Jul 21. J Med Chem. 2020. PMID: 32551603
Transaminases Provide Key Chiral Building Blocks for the Synthesis of Selective M1/M4 Agonists.
Thomson CG, Boss K, Calhoun A, Fridrich C, Gardinier KM, Hall EC, Jendza K, Kirman L, Labbé-Giguere N, Laumen K, Qian M, Sanyal S, Shultz MD, Snajdrova R, Tan K, Wang KY, Yang F, Gao F, Hong T, Dale E, Kuzmiski B, Ortuno D, Palacios DS. Thomson CG, et al. Among authors: fridrich c. ACS Med Chem Lett. 2023 Nov 6;14(12):1692-1699. doi: 10.1021/acsmedchemlett.3c00331. eCollection 2023 Dec 14. ACS Med Chem Lett. 2023. PMID: 38116445
Staging for Breast Cancer: A Comparison Between Old and New Approaches.
Kirn V, Bors S, Fridrich C, Schumacher C, Thangarajah F. Kirn V, et al. Among authors: fridrich c. Cancer Diagn Progn. 2023 Nov 3;3(6):673-677. doi: 10.21873/cdp.10271. eCollection 2023 Nov-Dec. Cancer Diagn Progn. 2023. PMID: 37927808 Free PMC article.
Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia.
Varkaris A, Pazolli E, Gunaydin H, Wang Q, Pierce L, Boezio AA, Bulku A, DiPietro L, Fridrich C, Frost A, Giordanetto F, Hamilton EP, Harris K, Holliday M, Hunter TL, Iskandar A, Ji Y, Larivée A, LaRochelle JR, Lescarbeau A, Llambi F, Lormil B, Mader MM, Mar BG, Martin I, McLean TH, Michelsen K, Pechersky Y, Puente-Poushnejad E, Raynor K, Rogala D, Samadani R, Schram AM, Shortsleeves K, Swaminathan S, Tajmir S, Tan G, Tang Y, Valverde R, Wehrenberg B, Wilbur J, Williams BR, Zeng H, Zhang H, Walters WP, Wolf BB, Shaw DE, Bergstrom DA, Watters J, Fraser JS, Fortin PD, Kipp DR. Varkaris A, et al. Among authors: fridrich c. Cancer Discov. 2024 Feb 8;14(2):240-257. doi: 10.1158/2159-8290.CD-23-0944. Cancer Discov. 2024. PMID: 37916956 Free PMC article.
17 results