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2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice.
Johansson L, Fotsch C, Bartberger MD, Castro VM, Chen M, Emery M, Gustafsson S, Hale C, Hickman D, Homan E, Jordan SR, Komorowski R, Li A, McRae K, Moniz G, Matsumoto G, Orihuela C, Palm G, Veniant M, Wang M, Williams M, Zhang J. Johansson L, et al. Among authors: homan e. J Med Chem. 2008 May 22;51(10):2933-43. doi: 10.1021/jm701551j. Epub 2008 Apr 18. J Med Chem. 2008. PMID: 18419108
Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1.
Llona-Minguez S, Höglund A, Wiita E, Almlöf I, Mateus A, Calderón-Montaño JM, Cazares-Körner C, Homan E, Loseva O, Baranczewski P, Jemth AS, Häggblad M, Martens U, Lundgren B, Artursson P, Lundbäck T, Jenmalm Jensen A, Warpman Berglund U, Scobie M, Helleday T. Llona-Minguez S, et al. Among authors: homan e. J Med Chem. 2017 Mar 9;60(5):2148-2154. doi: 10.1021/acs.jmedchem.6b01786. Epub 2017 Feb 15. J Med Chem. 2017. PMID: 28145708
Piperazin-1-ylpyridazine Derivatives Are a Novel Class of Human dCTP Pyrophosphatase 1 Inhibitors.
Llona-Minguez S, Höglund A, Ghassemian A, Desroses M, Calderón-Montaño JM, Burgos Morón E, Valerie NCK, Wiita E, Almlöf I, Koolmeister T, Mateus A, Cazares-Körner C, Sanjiv K, Homan E, Loseva O, Baranczewski P, Darabi M, Mehdizadeh A, Fayezi S, Jemth AS, Warpman Berglund U, Sigmundsson K, Lundbäck T, Jenmalm Jensen A, Artursson P, Scobie M, Helleday T. Llona-Minguez S, et al. Among authors: homan e. J Med Chem. 2017 May 25;60(10):4279-4292. doi: 10.1021/acs.jmedchem.7b00182. Epub 2017 May 16. J Med Chem. 2017. PMID: 28508636
Crystal structures of NUDT15 variants enabled by a potent inhibitor reveal the structural basis for thiopurine sensitivity.
Rehling D, Zhang SM, Jemth AS, Koolmeister T, Throup A, Wallner O, Scaletti E, Moriyama T, Nishii R, Davies J, Desroses M, Rudd SG, Scobie M, Homan E, Berglund UW, Yang JJ, Helleday T, Stenmark P. Rehling D, et al. Among authors: homan e. J Biol Chem. 2021 Jan-Jun;296:100568. doi: 10.1016/j.jbc.2021.100568. Epub 2021 Mar 19. J Biol Chem. 2021. PMID: 33753169 Free PMC article.
Target 2035 - an update on private sector contributions.
Ackloo S, Antolin AA, Bartolome JM, Beck H, Bullock A, Betz UAK, Böttcher J, Brown PJ, Chaturvedi M, Crisp A, Daniels D, Dreher J, Edfeldt K, Edwards AM, Egner U, Elkins J, Fischer C, Glendorf T, Goldberg S, Hartung IV, Hillisch A, Homan E, Knapp S, Köster M, Krämer O, Llaveria J, Lessel U, Lindemann S, Linderoth L, Matsui H, Michel M, Montel F, Mueller-Fahrnow A, Müller S, Owen DR, Saikatendu KS, Santhakumar V, Sanderson W, Scholten C, Schapira M, Sharma S, Shireman B, Sundström M, Todd MH, Tredup C, Venable J, Willson TM, Arrowsmith CH. Ackloo S, et al. Among authors: homan e. RSC Med Chem. 2023 Mar 16;14(6):1002-1011. doi: 10.1039/d2md00441k. eCollection 2023 Jun 22. RSC Med Chem. 2023. PMID: 37360399 Free PMC article.
41 results