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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: liras s. J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22196621
Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting.
Huard K, Smith AC, Cappon G, Dow RL, Edmonds DJ, El-Kattan A, Esler WP, Fernando DP, Griffith DA, Kalgutkar AS, Ross TT, Bagley SW, Beebe D, Bi YA, Cabral S, Crowley C, Doran SD, Dowling MS, Liras S, Mascitti V, Niosi M, Pfefferkorn JA, Polivkova J, Préville C, Price DA, Shavnya A, Shirai N, Smith AH, Southers JR, Tess DA, Thuma BA, Varma MV, Yang X. Huard K, et al. Among authors: liras s. J Med Chem. 2020 Oct 8;63(19):10879-10896. doi: 10.1021/acs.jmedchem.0c00640. Epub 2020 Sep 18. J Med Chem. 2020. PMID: 32809824
Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.
Darout E, Robinson RP, McClure KF, Corbett M, Li B, Shavnya A, Andrews MP, Jones CS, Li Q, Minich ML, Mascitti V, Guimarães CR, Munchhof MJ, Bahnck KB, Cai C, Price DA, Liras S, Bonin PD, Cornelius P, Wang R, Bagdasarian V, Sobota CP, Hornby S, Masterson VM, Joseph RM, Kalgutkar AS, Chen Y. Darout E, et al. Among authors: liras s. J Med Chem. 2013 Jan 10;56(1):301-19. doi: 10.1021/jm301626p. Epub 2012 Dec 31. J Med Chem. 2013. PMID: 23234271
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: liras s. 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: liras s. 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
Discovery of Potent and Orally Bioavailable Macrocyclic Peptide-Peptoid Hybrid CXCR7 Modulators.
Boehm M, Beaumont K, Jones R, Kalgutkar AS, Zhang L, Atkinson K, Bai G, Brown JA, Eng H, Goetz GH, Holder BR, Khunte B, Lazzaro S, Limberakis C, Ryu S, Shapiro MJ, Tylaska L, Yan J, Turner R, Leung SSF, Ramaseshan M, Price DA, Liras S, Jacobson MP, Earp DJ, Lokey RS, Mathiowetz AM, Menhaji-Klotz E. Boehm M, et al. Among authors: liras s. J Med Chem. 2017 Dec 14;60(23):9653-9663. doi: 10.1021/acs.jmedchem.7b01028. Epub 2017 Oct 30. J Med Chem. 2017. PMID: 29045152 Free article.
Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents.
Londregan AT, Wei L, Xiao J, Lintner NG, Petersen D, Dullea RG, McClure KF, Bolt MW, Warmus JS, Coffey SB, Limberakis C, Genovino J, Thuma BA, Hesp KD, Aspnes GE, Reidich B, Salatto CT, Chabot JR, Cate JHD, Liras S, Piotrowski DW. Londregan AT, et al. Among authors: liras s. J Med Chem. 2018 Jul 12;61(13):5704-5718. doi: 10.1021/acs.jmedchem.8b00650. Epub 2018 Jun 25. J Med Chem. 2018. PMID: 29878763
59 results