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N-Thiazolylamide-based free fatty-acid 2 receptor agonists: Discovery, lead optimization and demonstration of off-target effect in a diabetes model.
Hoveyda HR, Fraser GL, Zoute L, Dutheuil G, Schils D, Brantis C, Lapin A, Parcq J, Guitard S, Lenoir F, Bousmaqui ME, Rorive S, Hospied S, Blanc S, Bernard J, Ooms F, McNelis JC, Olefsky JM. Hoveyda HR, et al. Among authors: fraser gl. Bioorg Med Chem. 2018 Oct 1;26(18):5169-5180. doi: 10.1016/j.bmc.2018.09.015. Epub 2018 Sep 18. Bioorg Med Chem. 2018. PMID: 30253886
Optimization of the potency and pharmacokinetic properties of a macrocyclic ghrelin receptor agonist (Part I): Development of ulimorelin (TZP-101) from hit to clinic.
Hoveyda HR, Marsault E, Gagnon R, Mathieu AP, Vézina M, Landry A, Wang Z, Benakli K, Beaubien S, Saint-Louis C, Brassard M, Pinault JF, Ouellet L, Bhat S, Ramaseshan M, Peng X, Foucher L, Beauchemin S, Bhérer P, Veber DF, Peterson ML, Fraser GL. Hoveyda HR, et al. Among authors: fraser gl. J Med Chem. 2011 Dec 22;54(24):8305-20. doi: 10.1021/jm2007062. Epub 2011 Nov 22. J Med Chem. 2011. PMID: 22106937
Expression of Free Fatty Acid Receptor 2 by Dendritic Cells Prevents Their Expression of Interleukin 27 and Is Required for Maintenance of Mucosal Barrier and Immune Response Against Colorectal Tumors in Mice.
Lavoie S, Chun E, Bae S, Brennan CA, Gallini Comeau CA, Lang JK, Michaud M, Hoveyda HR, Fraser GL, Fuller MH, Layden BT, Glickman JN, Garrett WS. Lavoie S, et al. Among authors: fraser gl. Gastroenterology. 2020 Apr;158(5):1359-1372.e9. doi: 10.1053/j.gastro.2019.12.027. Epub 2020 Jan 7. Gastroenterology. 2020. PMID: 31917258 Free PMC article.
Discovery of a new class of macrocyclic antagonists to the human motilin receptor.
Marsault E, Hoveyda HR, Peterson ML, Saint-Louis C, Landry A, Vézina M, Ouellet L, Wang Z, Ramaseshan M, Beaubien S, Benakli K, Beauchemin S, Déziel R, Peeters T, Fraser GL. Marsault E, et al. Among authors: fraser gl. J Med Chem. 2006 Nov 30;49(24):7190-7. doi: 10.1021/jm0606600. J Med Chem. 2006. PMID: 17125271
145 results