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From a Cone Snail Toxin to a Competitive MC4R Antagonist.
Reynaud S, Laurin SA, Ciolek J, Barbe P, Van Baelen AC, Susset M, Blondel F, Ghazarian M, Boeri J, Vanden Driessche M, Upert G, Mourier G, Kessler P, Konnert L, Beroud R, Keck M, Servent D, Bouvier M, Gilles N. Reynaud S, et al. Among authors: bouvier m. J Med Chem. 2022 Sep 22;65(18):12084-12094. doi: 10.1021/acs.jmedchem.2c00786. Epub 2022 Sep 5. J Med Chem. 2022. PMID: 36063022
Human MC4R variants affect endocytosis, trafficking and dimerization revealing multiple cellular mechanisms involved in weight regulation.
Brouwers B, de Oliveira EM, Marti-Solano M, Monteiro FBF, Laurin SA, Keogh JM, Henning E, Bounds R, Daly CA, Houston S, Ayinampudi V, Wasiluk N, Clarke D, Plouffe B, Bouvier M, Babu MM, Farooqi IS, Mokrosiński J. Brouwers B, et al. Among authors: bouvier m. Cell Rep. 2021 Mar 23;34(12):108862. doi: 10.1016/j.celrep.2021.108862. Cell Rep. 2021. PMID: 33761344 Free PMC article.
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: bouvier m. 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
Size-Reduced Macrocyclic Analogues of [Pyr1]-apelin-13 Showing Negative Gα12 Bias Still Produce Prolonged Cardiac Effects.
Tran K, Sainsily X, Côté J, Coquerel D, Couvineau P, Saibi S, Haroune L, Besserer-Offroy É, Flynn-Robitaille J, Resua Rojas M, Murza A, Longpré JM, Auger-Messier M, Lesur O, Bouvier M, Marsault É, Boudreault PL, Sarret P. Tran K, et al. Among authors: bouvier m. J Med Chem. 2022 Jan 13;65(1):531-551. doi: 10.1021/acs.jmedchem.1c01708. Epub 2022 Jan 4. J Med Chem. 2022. PMID: 34982553
793 results