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A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor.
Griffith DA, Edmonds DJ, Fortin JP, Kalgutkar AS, Kuzmiski JB, Loria PM, Saxena AR, Bagley SW, Buckeridge C, Curto JM, Derksen DR, Dias JM, Griffor MC, Han S, Jackson VM, Landis MS, Lettiere D, Limberakis C, Liu Y, Mathiowetz AM, Patel JC, Piotrowski DW, Price DA, Ruggeri RB, Tess DA. Griffith DA, et al. Among authors: limberakis c. J Med Chem. 2022 Jun 23;65(12):8208-8226. doi: 10.1021/acs.jmedchem.1c01856. Epub 2022 Jun 1. J Med Chem. 2022. PMID: 35647711 Free PMC article.
Maximizing lipophilic efficiency: the use of Free-Wilson analysis in the design of inhibitors of acetyl-CoA carboxylase.
Freeman-Cook KD, Amor P, Bader S, Buzon LM, Coffey SB, Corbett JW, Dirico KJ, Doran SD, Elliott RL, Esler W, Guzman-Perez A, Henegar KE, Houser JA, Jones CS, Limberakis C, Loomis K, McPherson K, Murdande S, Nelson KL, Phillion D, Pierce BS, Song W, Sugarman E, Tapley S, Tu M, Zhao Z. Freeman-Cook KD, et al. Among authors: limberakis c. J Med Chem. 2012 Jan 26;55(2):935-42. doi: 10.1021/jm201503u. Epub 2012 Jan 11. J Med Chem. 2012. PMID: 22148323
Demonstration of the innate electrophilicity of 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine (BETP), a small-molecule positive allosteric modulator of the glucagon-like peptide-1 receptor.
Eng H, Sharma R, McDonald TS, Edmonds DJ, Fortin JP, Li X, Stevens BD, Griffith DA, Limberakis C, Nolte WM, Price DA, Jackson M, Kalgutkar AS. Eng H, et al. Among authors: limberakis c. Drug Metab Dispos. 2013 Aug;41(8):1470-9. doi: 10.1124/dmd.113.052183. Epub 2013 May 7. Drug Metab Dispos. 2013. PMID: 23653442
Revisiting N-to-O acyl shift for synthesis of natural product-like cyclic depsipeptides.
Schwochert J, Pye C, Ahlbach C, Abdollahian Y, Farley K, Khunte B, Limberakis C, Kalgutkar AS, Eng H, Shapiro MJ, Mathiowetz AM, Price DA, Liras S, Lokey RS. Schwochert J, et al. Among authors: limberakis c. Org Lett. 2014 Dec 5;16(23):6088-91. doi: 10.1021/ol503170b. Epub 2014 Nov 20. Org Lett. 2014. PMID: 25412436
Decreasing the rate of metabolic ketone reduction in the discovery of a clinical acetyl-CoA carboxylase inhibitor for the treatment of diabetes.
Griffith DA, Kung DW, Esler WP, Amor PA, Bagley SW, Beysen C, Carvajal-Gonzalez S, Doran SD, Limberakis C, Mathiowetz AM, McPherson K, Price DA, Ravussin E, Sonnenberg GE, Southers JA, Sweet LJ, Turner SM, Vajdos FF. Griffith DA, et al. Among authors: limberakis c. J Med Chem. 2014 Dec 26;57(24):10512-26. doi: 10.1021/jm5016022. Epub 2014 Dec 11. J Med Chem. 2014. PMID: 25423286 Free PMC article. Clinical Trial.
Short Hydrophobic Peptides with Cyclic Constraints Are Potent Glucagon-like Peptide-1 Receptor (GLP-1R) Agonists.
Hoang HN, Song K, Hill TA, Derksen DR, Edmonds DJ, Kok WM, Limberakis C, Liras S, Loria PM, Mascitti V, Mathiowetz AM, Mitchell JM, Piotrowski DW, Price DA, Stanton RV, Suen JY, Withka JM, Griffith DA, Fairlie DP. Hoang HN, et al. Among authors: limberakis c. J Med Chem. 2015 May 14;58(9):4080-5. doi: 10.1021/acs.jmedchem.5b00166. Epub 2015 Apr 16. J Med Chem. 2015. PMID: 25839426
37 results