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Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.
Trân K, Van Den Hauwe R, Sainsily X, Couvineau P, Côté J, Simard L, Echevarria M, Murza A, Serre A, Théroux L, Saibi S, Haroune L, Longpré JM, Lesur O, Auger-Messier M, Spino C, Bouvier M, Sarret P, Ballet S, Marsault É. Trân K, et al. Among authors: marsault e. J Med Chem. 2021 May 13;64(9):5345-5364. doi: 10.1021/acs.jmedchem.0c01941. Epub 2021 Feb 1. J Med Chem. 2021. PMID: 33524256
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: marsault e. J Med Chem. 2011 Dec 22;54(24):8305-20. doi: 10.1021/jm2007062. Epub 2011 Nov 22. J Med Chem. 2011. PMID: 22106937
Discovery and Structure-Activity Relationship of a Bioactive Fragment of ELABELA that Modulates Vascular and Cardiac Functions.
Murza A, Sainsily X, Coquerel D, Côté J, Marx P, Besserer-Offroy É, Longpré JM, Lainé J, Reversade B, Salvail D, Leduc R, Dumaine R, Lesur O, Auger-Messier M, Sarret P, Marsault É. Murza A, et al. Among authors: marsault e. J Med Chem. 2016 Apr 14;59(7):2962-72. doi: 10.1021/acs.jmedchem.5b01549. Epub 2016 Mar 30. J Med Chem. 2016. PMID: 26986036
77 results