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PPARγ Corepression Involves Alternate Ligand Conformation and Inflation of H12 Ensembles.
Frkic RL, Pederick JL, Horsfall AJ, Jovcevski B, Crame EE, Kowalczyk W, Pukala TL, Chang MR, Zheng J, Blayo AL, Abell AD, Kamenecka TM, Harbort JS, Harmer JR, Griffin PR, Bruning JB. Frkic RL, et al. Among authors: blayo al. ACS Chem Biol. 2023 May 19;18(5):1115-1123. doi: 10.1021/acschembio.2c00917. Epub 2023 May 5. ACS Chem Biol. 2023. PMID: 37146157
Development of Nonpeptidic Inverse Agonists of the Ghrelin Receptor (GHSR) Based on the 1,2,4-Triazole Scaffold.
Haj Salah KB, Maingot M, Blayo AL, M'Kadmi C, Damian M, Mary S, Cantel S, Neasta J, Oiry C, Péraldi-Roux S, Fernandez G, Romero GG, Perello M, Marie J, Banères JL, Fehrentz JA, Denoyelle S. Haj Salah KB, et al. Among authors: blayo al. J Med Chem. 2020 Oct 8;63(19):10796-10815. doi: 10.1021/acs.jmedchem.9b02122. Epub 2020 Sep 21. J Med Chem. 2020. PMID: 32882134
A structural mechanism for directing corepressor-selective inverse agonism of PPARγ.
Brust R, Shang J, Fuhrmann J, Mosure SA, Bass J, Cano A, Heidari Z, Chrisman IM, Nemetchek MD, Blayo AL, Griffin PR, Kamenecka TM, Hughes TS, Kojetin DJ. Brust R, et al. Among authors: blayo al. Nat Commun. 2018 Nov 8;9(1):4687. doi: 10.1038/s41467-018-07133-w. Nat Commun. 2018. PMID: 30409975 Free PMC article.
Defining a conformational ensemble that directs activation of PPARγ.
Chrisman IM, Nemetchek MD, de Vera IMS, Shang J, Heidari Z, Long Y, Reyes-Caballero H, Galindo-Murillo R, Cheatham TE 3rd, Blayo AL, Shin Y, Fuhrmann J, Griffin PR, Kamenecka TM, Kojetin DJ, Hughes TS. Chrisman IM, et al. Among authors: blayo al. Nat Commun. 2018 May 4;9(1):1794. doi: 10.1038/s41467-018-04176-x. Nat Commun. 2018. PMID: 29728618 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. Among authors: blayo 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
Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists.
Asteian A, Blayo AL, He Y, Koenig M, Shin Y, Kuruvilla DS, Corzo CA, Cameron MD, Lin L, Ruiz C, Khan S, Kumar N, Busby S, Marciano DP, Garcia-Ordonez RD, Griffin PR, Kamenecka TM. Asteian A, et al. Among authors: blayo al. ACS Med Chem Lett. 2015 Aug 4;6(9):998-1003. doi: 10.1021/acsmedchemlett.5b00218. eCollection 2015 Sep 10. ACS Med Chem Lett. 2015. PMID: 26396687 Free PMC article.
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