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Page 1
Efficient Liver Targeting by Polyvalent Display of a Compact Ligand for the Asialoglycoprotein Receptor.
Sanhueza CA, Baksh MM, Thuma B, Roy MD, Dutta S, Préville C, Chrunyk BA, Beaumont K, Dullea R, Ammirati M, Liu S, Gebhard D, Finley JE, Salatto CT, King-Ahmad A, Stock I, Atkinson K, Reidich B, Lin W, Kumar R, Tu M, Menhaji-Klotz E, Price DA, Liras S, Finn MG, Mascitti V. Sanhueza CA, et al. Among authors: liras s. J Am Chem Soc. 2017 Mar 8;139(9):3528-3536. doi: 10.1021/jacs.6b12964. Epub 2017 Feb 23. J Am Chem Soc. 2017. PMID: 28230359 Free PMC article.
Receptor-Mediated Delivery of CRISPR-Cas9 Endonuclease for Cell-Type-Specific Gene Editing.
Rouet R, Thuma BA, Roy MD, Lintner NG, Rubitski DM, Finley JE, Wisniewska HM, Mendonsa R, Hirsh A, de Oñate L, Compte Barrón J, McLellan TJ, Bellenger J, Feng X, Varghese A, Chrunyk BA, Borzilleri K, Hesp KD, Zhou K, Ma N, Tu M, Dullea R, McClure KF, Wilson RC, Liras S, Mascitti V, Doudna JA. Rouet R, et al. Among authors: liras s. J Am Chem Soc. 2018 May 30;140(21):6596-6603. doi: 10.1021/jacs.8b01551. Epub 2018 May 18. J Am Chem Soc. 2018. PMID: 29668265 Free PMC article.
Liver-Targeted Small-Molecule Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9 Synthesis.
McClure KF, Piotrowski DW, Petersen D, Wei L, Xiao J, Londregan AT, Kamlet AS, Dechert-Schmitt AM, Raymer B, Ruggeri RB, Canterbury D, Limberakis C, Liras S, DaSilva-Jardine P, Dullea RG, Loria PM, Reidich B, Salatto CT, Eng H, Kimoto E, Atkinson K, King-Ahmad A, Scott D, Beaumont K, Chabot JR, Bolt MW, Maresca K, Dahl K, Arakawa R, Takano A, Halldin C. McClure KF, et al. Among authors: liras s. Angew Chem Int Ed Engl. 2017 Dec 18;56(51):16218-16222. doi: 10.1002/anie.201708744. Epub 2017 Nov 24. Angew Chem Int Ed Engl. 2017. PMID: 29073340
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
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
Design and synthesis of truncated EGF-A peptides that restore LDL-R recycling in the presence of PCSK9 in vitro.
Schroeder CI, Swedberg JE, Withka JM, Rosengren KJ, Akcan M, Clayton DJ, Daly NL, Cheneval O, Borzilleri KA, Griffor M, Stock I, Colless B, Walsh P, Sunderland P, Reyes A, Dullea R, Ammirati M, Liu S, McClure KF, Tu M, Bhattacharya SK, Liras S, Price DA, Craik DJ. Schroeder CI, et al. Among authors: liras s. Chem Biol. 2014 Feb 20;21(2):284-94. doi: 10.1016/j.chembiol.2013.11.014. Epub 2014 Jan 16. Chem Biol. 2014. PMID: 24440079
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.
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
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