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Page 1
Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.
Pfefferkorn JA, Guzman-Perez A, Litchfield J, Aiello R, Treadway JL, Pettersen J, Minich ML, Filipski KJ, Jones CS, Tu M, Aspnes G, Risley H, Bian J, Stevens BD, Bourassa P, D'Aquila T, Baker L, Barucci N, Robertson AS, Bourbonais F, Derksen DR, Macdougall M, Cabrera O, Chen J, Lapworth AL, Landro JA, Zavadoski WJ, Atkinson K, Haddish-Berhane N, Tan B, Yao L, Kosa RE, Varma MV, Feng B, Duignan DB, El-Kattan A, Murdande S, Liu S, Ammirati M, Knafels J, Dasilva-Jardine P, Sweet L, Liras S, Rolph TP. Pfefferkorn JA, et al. Among authors: derksen dr. J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22196621
The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of type 2 diabetes mellitus.
Pfefferkorn JA, Tu M, Filipski KJ, Guzman-Perez A, Bian J, Aspnes GE, Sammons MF, Song W, Li JC, Jones CS, Patel L, Rasmusson T, Zeng D, Karki K, Hamilton M, Hank R, Atkinson K, Litchfield J, Aiello R, Baker L, Barucci N, Bourassa P, Bourbonais F, D'Aquila T, Derksen DR, MacDougall M, Robertson A. Pfefferkorn JA, et al. Among authors: derksen dr. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7100-5. doi: 10.1016/j.bmcl.2012.09.082. Epub 2012 Sep 29. Bioorg Med Chem Lett. 2012. PMID: 23089526
Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif.
Filipski KJ, Guzman-Perez A, Bian J, Perreault C, Aspnes GE, Didiuk MT, Dow RL, Hank RF, Jones CS, Maguire RJ, Tu M, Zeng D, Liu S, Knafels JD, Litchfield J, Atkinson K, Derksen DR, Bourbonais F, Gajiwala KS, Hickey M, Johnson TO, Humphries PS, Pfefferkorn JA. Filipski KJ, et al. Among authors: derksen dr. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4571-8. doi: 10.1016/j.bmcl.2013.06.036. Epub 2013 Jun 20. Bioorg Med Chem Lett. 2013. PMID: 23831135
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.
Stevens BD, Litchfield J, Pfefferkorn JA, Atkinson K, Perreault C, Amor P, Bahnck K, Berliner MA, Calloway J, Carlo A, Derksen DR, Filipski KJ, Gumkowski M, Jassal C, MacDougall M, Murphy B, Nkansah P, Pettersen J, Rotter C, Zhang Y. Stevens BD, et al. Among authors: derksen dr. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6588-92. doi: 10.1016/j.bmcl.2013.10.057. Epub 2013 Nov 4. Bioorg Med Chem Lett. 2013. PMID: 24239482
Cyclic alpha-conotoxin peptidomimetic chimeras as potent GLP-1R agonists.
Swedberg JE, Schroeder CI, Mitchell JM, Durek T, Fairlie DP, Edmonds DJ, Griffith DA, Ruggeri RB, Derksen DR, Loria PM, Liras S, Price DA, Craik DJ. Swedberg JE, et al. Among authors: derksen dr. Eur J Med Chem. 2015 Oct 20;103:175-84. doi: 10.1016/j.ejmech.2015.08.046. Epub 2015 Aug 29. Eur J Med Chem. 2015. PMID: 26352676
Helixconstraints and amino acid substitution in GLP-1 increase cAMP and insulin secretion but not beta-arrestin 2 signaling.
Plisson F, Hill TA, Mitchell JM, Hoang HN, de Araujo AD, Xu W, Cotterell A, Edmonds DJ, Stanton RV, Derksen DR, Loria PM, Griffith DA, Price DA, Liras S, Fairlie DP. Plisson F, et al. Among authors: derksen dr. Eur J Med Chem. 2017 Feb 15;127:703-714. doi: 10.1016/j.ejmech.2016.10.044. Epub 2016 Oct 21. Eur J Med Chem. 2017. PMID: 27823886
Truncated Glucagon-like Peptide-1 and Exendin-4 α-Conotoxin pl14a Peptide Chimeras Maintain Potency and α-Helicity and Reveal Interactions Vital for cAMP Signaling in Vitro.
Swedberg JE, Schroeder CI, Mitchell JM, Fairlie DP, Edmonds DJ, Griffith DA, Ruggeri RB, Derksen DR, Loria PM, Price DA, Liras S, Craik DJ. Swedberg JE, et al. Among authors: derksen dr. J Biol Chem. 2016 Jul 22;291(30):15778-87. doi: 10.1074/jbc.M116.724542. Epub 2016 May 10. J Biol Chem. 2016. PMID: 27226591 Free PMC article.
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: derksen dr. 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.
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: derksen dr. 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
Optimization of amide-based EP3 receptor antagonists.
Lee EC, Futatsugi K, Arcari JT, Bahnck K, Coffey SB, Derksen DR, Kalgutkar AS, Loria PM, Sharma R. Lee EC, et al. Among authors: derksen dr. Bioorg Med Chem Lett. 2016 Jun 1;26(11):2670-5. doi: 10.1016/j.bmcl.2016.04.009. Epub 2016 Apr 9. Bioorg Med Chem Lett. 2016. PMID: 27107947
17 results