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Page 1
Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF.
Shao W, Mishina YM, Feng Y, Caponigro G, Cooke VG, Rivera S, Wang Y, Shen F, Korn JM, Mathews Griner LA, Nishiguchi G, Rico A, Tellew J, Haling JR, Aversa R, Polyakov V, Zang R, Hekmat-Nejad M, Amiri P, Singh M, Keen N, Dillon MP, Lees E, Ramurthy S, Sellers WR, Stuart DD. Shao W, et al. Among authors: mishina ym. Cancer Res. 2018 Mar 15;78(6):1537-1548. doi: 10.1158/0008-5472.CAN-17-2033. Epub 2018 Jan 17. Cancer Res. 2018. PMID: 29343524
Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic.
Ramurthy S, Taft BR, Aversa RJ, Barsanti PA, Burger MT, Lou Y, Nishiguchi GA, Rico A, Setti L, Smith A, Subramanian S, Tamez V, Tanner H, Wan L, Hu C, Appleton BA, Mamo M, Tandeske L, Tellew JE, Huang S, Yue Q, Chaudhary A, Tian H, Iyer R, Hassan AQ, Mathews Griner LA, La Bonte LR, Cooke VG, Van Abbema A, Merritt H, Gampa K, Feng F, Yuan J, Mishina Y, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Sellers WR, Lees E, Shao W, Dillon MP, Stuart DD. Ramurthy S, et al. J Med Chem. 2020 Mar 12;63(5):2013-2027. doi: 10.1021/acs.jmedchem.9b00161. Epub 2019 May 16. J Med Chem. 2020. PMID: 31059256
LXH254, a Potent and Selective ARAF-Sparing Inhibitor of BRAF and CRAF for the Treatment of MAPK-Driven Tumors.
Monaco KA, Delach S, Yuan J, Mishina Y, Fordjour P, Labrot E, McKay D, Guo R, Higgins S, Wang HQ, Liang J, Bui K, Green J, Aspesi P, Ambrose J, Mapa F, Griner L, Jaskelioff M, Fuller J, Crawford K, Pardee G, Widger S, Hammerman PS, Engelman JA, Stuart DD, Cooke VG, Caponigro G. Monaco KA, et al. Clin Cancer Res. 2021 Apr 1;27(7):2061-2073. doi: 10.1158/1078-0432.CCR-20-2563. Epub 2020 Dec 22. Clin Cancer Res. 2021. PMID: 33355204
Inhibition of prenylated KRAS in a lipid environment.
Jansen JM, Wartchow C, Jahnke W, Fong S, Tsang T, Pfister K, Zavorotinskaya T, Bussiere D, Cheng JM, Crawford K, Dai Y, Dove J, Fang E, Feng Y, Florent JM, Fuller J, Gossert AD, Hekmat-Nejad M, Henry C, Klopp J, Lenahan WP, Lingel A, Ma S, Meyer A, Mishina Y, Narberes J, Pardee G, Ramurthy S, Rieffel S, Stuart D, Subramanian S, Tandeske L, Widger S, Widmer A, Winterhalter A, Zaror I, Hardy S. Jansen JM, et al. PLoS One. 2017 Apr 6;12(4):e0174706. doi: 10.1371/journal.pone.0174706. eCollection 2017. PLoS One. 2017. PMID: 28384226 Free PMC article.
Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight.
Touré BB, Giraldes J, Smith T, Sprague ER, Wang Y, Mathieu S, Chen Z, Mishina Y, Feng Y, Yan-Neale Y, Shakya S, Chen D, Meyer M, Puleo D, Brazell JT, Straub C, Sage D, Wright K, Yuan Y, Chen X, Duca J, Kim S, Tian L, Martin E, Hurov K, Shao W. Touré BB, et al. J Med Chem. 2016 May 26;59(10):4711-23. doi: 10.1021/acs.jmedchem.6b00052. Epub 2016 May 17. J Med Chem. 2016. PMID: 27187609
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
Tria GS, Abrams T, Baird J, Burks HE, Firestone B, Gaither LA, Hamann LG, He G, Kirby CA, Kim S, Lombardo F, Macchi KJ, McDonnell DP, Mishina Y, Norris JD, Nunez J, Springer C, Sun Y, Thomsen NM, Wang C, Wang J, Yu B, Tiong-Yip CL, Peukert S. Tria GS, et al. J Med Chem. 2018 Apr 12;61(7):2837-2864. doi: 10.1021/acs.jmedchem.7b01682. Epub 2018 Mar 22. J Med Chem. 2018. PMID: 29562737
Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling.
Huang SM, Mishina YM, Liu S, Cheung A, Stegmeier F, Michaud GA, Charlat O, Wiellette E, Zhang Y, Wiessner S, Hild M, Shi X, Wilson CJ, Mickanin C, Myer V, Fazal A, Tomlinson R, Serluca F, Shao W, Cheng H, Shultz M, Rau C, Schirle M, Schlegl J, Ghidelli S, Fawell S, Lu C, Curtis D, Kirschner MW, Lengauer C, Finan PM, Tallarico JA, Bouwmeester T, Porter JA, Bauer A, Cong F. Huang SM, et al. Among authors: mishina ym. Nature. 2009 Oct 1;461(7264):614-20. doi: 10.1038/nature08356. Epub 2009 Sep 16. Nature. 2009. PMID: 19759537
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.
Burks HE, Abrams T, Kirby CA, Baird J, Fekete A, Hamann LG, Kim S, Lombardo F, Loo A, Lubicka D, Macchi K, McDonnell DP, Mishina Y, Norris JD, Nunez J, Saran C, Sun Y, Thomsen NM, Wang C, Wang J, Peukert S. Burks HE, et al. J Med Chem. 2017 Apr 13;60(7):2790-2818. doi: 10.1021/acs.jmedchem.6b01468. Epub 2017 Mar 15. J Med Chem. 2017. PMID: 28296398
266 results