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New trisubstituted 1,2,4-triazoles as ghrelin receptor antagonists.
Blayo AL, Maingot M, Aicher B, M'Kadmi C, Schmidt P, Müller G, Teifel M, Günther E, Gagne D, Denoyelle S, Martinez J, Fehrentz JA. Blayo AL, et al. Bioorg Med Chem Lett. 2015 Jan 1;25(1):20-4. doi: 10.1016/j.bmcl.2014.11.031. Epub 2014 Nov 15. Bioorg Med Chem Lett. 2015. PMID: 25435152
Agonism, Antagonism, and Inverse Agonism Bias at the Ghrelin Receptor Signaling.
M'Kadmi C, Leyris JP, Onfroy L, Galés C, Saulière A, Gagne D, Damian M, Mary S, Maingot M, Denoyelle S, Verdié P, Fehrentz JA, Martinez J, Banères JL, Marie J. M'Kadmi C, et al. J Biol Chem. 2015 Nov 6;290(45):27021-27039. doi: 10.1074/jbc.M115.659250. Epub 2015 Sep 11. J Biol Chem. 2015. PMID: 26363071 Free PMC article.
New ligands of the ghrelin receptor based on the 1,2,4-triazole scaffold by introduction of a second chiral center.
Maingot M, Blayo AL, Denoyelle S, M'Kadmi C, Damian M, Mary S, Gagne D, Sanchez P, Aicher B, Schmidt P, Müller G, Teifel M, Günther E, Marie J, Banères JL, Martinez J, Fehrentz JA. Maingot M, et al. Bioorg Med Chem Lett. 2016 May 15;26(10):2408-2412. doi: 10.1016/j.bmcl.2016.04.003. Epub 2016 Apr 4. Bioorg Med Chem Lett. 2016. PMID: 27072910
Ghrelin receptor conformational dynamics regulate the transition from a preassembled to an active receptor:Gq complex.
Damian M, Mary S, Maingot M, M'Kadmi C, Gagne D, Leyris JP, Denoyelle S, Gaibelet G, Gavara L, Garcia de Souza Costa M, Perahia D, Trinquet E, Mouillac B, Galandrin S, Galès C, Fehrentz JA, Floquet N, Martinez J, Marie J, Banères JL. Damian M, et al. Proc Natl Acad Sci U S A. 2015 Feb 3;112(5):1601-6. doi: 10.1073/pnas.1414618112. Epub 2015 Jan 20. Proc Natl Acad Sci U S A. 2015. PMID: 25605885 Free PMC article.
26 results