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Potent and Orally Bioavailable Inverse Agonists of RORγt Resulting from Structure-Based Design.
Narjes F, Xue Y, von Berg S, Malmberg J, Llinas A, Olsson RI, Jirholt J, Grindebacke H, Leffler A, Hossain N, Lepistö M, Thunberg L, Leek H, Aagaard A, McPheat J, Hansson EL, Bäck E, Tångefjord S, Chen R, Xiong Y, Hongbin G, Hansson TG. Narjes F, et al. J Med Chem. 2018 Sep 13;61(17):7796-7813. doi: 10.1021/acs.jmedchem.8b00783. Epub 2018 Aug 27. J Med Chem. 2018. PMID: 30095900
Discovery of (7R)-14-cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid (MK-3281), a potent and orally bioavailable finger-loop inhibitor of the hepatitis C virus NS5B polymerase.
Narjes F, Crescenzi B, Ferrara M, Habermann J, Colarusso S, Ferreira Mdel R, Stansfield I, Mackay AC, Conte I, Ercolani C, Zaramella S, Palumbi MC, Meuleman P, Leroux-Roels G, Giuliano C, Fiore F, Di Marco S, Baiocco P, Koch U, Migliaccio G, Altamura S, Laufer R, De Francesco R, Rowley M. Narjes F, et al. J Med Chem. 2011 Jan 13;54(1):289-301. doi: 10.1021/jm1013105. Epub 2010 Dec 8. J Med Chem. 2011. PMID: 21141896
HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase.
Evenäs J, Edfeldt F, Lepistö M, Svitacheva N, Synnergren A, Lundquist B, Gränse M, Rönnholm A, Varga M, Wright J, Wei M, Yue S, Wang J, Li C, Li X, Chen G, Liao Y, Lv G, Tjörnebo A, Narjes F. Evenäs J, et al. Among authors: narjes f. Bioorg Med Chem Lett. 2014 Mar 1;24(5):1315-21. doi: 10.1016/j.bmcl.2014.01.050. Epub 2014 Jan 28. Bioorg Med Chem Lett. 2014. PMID: 24508129
Benzoxazepines Achieve Potent Suppression of IL-17 Release in Human T-Helper 17 (TH 17) Cells through an Induced-Fit Binding Mode to the Nuclear Receptor RORγ.
Olsson RI, Xue Y, von Berg S, Aagaard A, McPheat J, Hansson EL, Bernström J, Hansson P, Jirholt J, Grindebacke H, Leffler A, Chen R, Xiong Y, Ge H, Hansson TG, Narjes F. Olsson RI, et al. Among authors: narjes f. ChemMedChem. 2016 Jan 19;11(2):207-16. doi: 10.1002/cmdc.201500432. Epub 2015 Nov 10. ChemMedChem. 2016. PMID: 26553345
Discovery of Potent and Orally Bioavailable Inverse Agonists of the Retinoic Acid Receptor-Related Orphan Receptor C2.
von Berg S, Xue Y, Collins M, Llinas A, Olsson RI, Halvarsson T, Lindskog M, Malmberg J, Jirholt J, Krutrök N, Ramnegård M, Brännström M, Lundqvist A, Lepistö M, Aagaard A, McPheat J, Hansson EL, Chen R, Xiong Y, Hansson TG, Narjes F. von Berg S, et al. Among authors: narjes f. ACS Med Chem Lett. 2019 May 29;10(6):972-977. doi: 10.1021/acsmedchemlett.9b00158. eCollection 2019 Jun 13. ACS Med Chem Lett. 2019. PMID: 31223457 Free PMC article.
AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2.
Narjes F, Llinas A, von Berg S, Jirholt J, Lever S, Pehrson R, Collins M, Malmberg A, Svanberg P, Xue Y, Olsson RI, Malmberg J, Hughes G, Hossain N, Grindebacke H, Leffler A, Krutrök N, Bäck E, Ramnegård M, Lepistö M, Thunberg L, Aagaard A, McPheat J, Hansson EL, Chen R, Xiong Y, Hansson TG. Narjes F, et al. J Med Chem. 2021 Sep 23;64(18):13807-13829. doi: 10.1021/acs.jmedchem.1c01197. Epub 2021 Aug 31. J Med Chem. 2021. PMID: 34464130
Discovery and Characterization of a Bicyclic Peptide (Bicycle) Binder to Thymic Stromal Lymphopoietin.
Narjes F, Edfeldt F, Petersen J, Öster L, Hamblet C, Bird J, Bold P, Rae R, Bäck E, Stomilovic S, Zlatoidsky P, Svensson T, Hidestål L, Kunalingam L, Shamovsky I, De Maria L, Gordon E, Lewis RJ, Watcham S, van Rietschoten K, Mudd GE, Harrison H, Chen L, Skynner MJ. Narjes F, et al. J Med Chem. 2024 Feb 8;67(3):2220-2235. doi: 10.1021/acs.jmedchem.3c02163. Epub 2024 Jan 29. J Med Chem. 2024. PMID: 38284169
53 results