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Page 1
An alternate binding site for PPARγ ligands.
Hughes TS, Giri PK, de Vera IM, Marciano DP, Kuruvilla DS, Shin Y, Blayo AL, Kamenecka TM, Burris TP, Griffin PR, Kojetin DJ. Hughes TS, et al. Among authors: blayo al. Nat Commun. 2014 Apr 7;5:3571. doi: 10.1038/ncomms4571. Nat Commun. 2014. PMID: 24705063 Free PMC article.
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.
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.
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.
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
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
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
14 results