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21,166 results

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Page 1
Identification of a novel conformationally constrained glucagon receptor antagonist.
Lee EC, Tu M, Stevens BD, Bian J, Aspnes G, Perreault C, Sammons MF, Wright SW, Litchfield J, Kalgutkar AS, Sharma R, Didiuk MT, Ebner DC, Filipski KJ, Brown J, Atkinson K, Pfefferkorn JA, Guzman-Perez A. Lee EC, et al. Among authors: brown j. Bioorg Med Chem Lett. 2014 Feb 1;24(3):839-44. doi: 10.1016/j.bmcl.2013.12.090. Epub 2013 Dec 28. Bioorg Med Chem Lett. 2014. PMID: 24418771
A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity.
Filipski KJ, Bian J, Ebner DC, Lee EC, Li JC, Sammons MF, Wright SW, Stevens BD, Didiuk MT, Tu M, Perreault C, Brown J, Atkinson K, Tan B, Salatto CT, Litchfield J, Pfefferkorn JA, Guzman-Perez A. Filipski KJ, et al. Among authors: brown j. Bioorg Med Chem Lett. 2012 Jan 1;22(1):415-20. doi: 10.1016/j.bmcl.2011.10.113. Epub 2011 Nov 6. Bioorg Med Chem Lett. 2012. PMID: 22119466
The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus.
Guzman-Perez A, Pfefferkorn JA, Lee EC, Stevens BD, Aspnes GE, Bian J, Didiuk MT, Filipski KJ, Moore D, Perreault C, Sammons MF, Tu M, Brown J, Atkinson K, Litchfield J, Tan B, Samas B, Zavadoski WJ, Salatto CT, Treadway J. Guzman-Perez A, et al. Among authors: brown j. Bioorg Med Chem Lett. 2013 May 15;23(10):3051-8. doi: 10.1016/j.bmcl.2013.03.014. Epub 2013 Mar 13. Bioorg Med Chem Lett. 2013. PMID: 23562063
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).
Edmonds DJ, Kung DW, Kalgutkar AS, Filipski KJ, Ebner DC, Cabral S, Smith AC, Aspnes GE, Bhattacharya SK, Borzilleri KA, Brown JA, Calabrese MF, Caspers NL, Cokorinos EC, Conn EL, Dowling MS, Eng H, Feng B, Fernando DP, Genung NE, Herr M, Kurumbail RG, Lavergne SY, Lee EC, Li Q, Mathialagan S, Miller RA, Panteleev J, Polivkova J, Rajamohan F, Reyes AR, Salatto CT, Shavnya A, Thuma BA, Tu M, Ward J, Withka JM, Xiao J, Cameron KO. Edmonds DJ, et al. Among authors: brown ja. J Med Chem. 2018 Mar 22;61(6):2372-2383. doi: 10.1021/acs.jmedchem.7b01641. Epub 2018 Feb 28. J Med Chem. 2018. PMID: 29466005
N-benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors.
Atkinson KA, Beretta EE, Brown JA, Castrodad M, Chen Y, Cosgrove JM, Du P, Litchfield J, Makowski M, Martin K, McLellan TJ, Neagu C, Perry DA, Piotrowski DW, Steppan CM, Trilles R. Atkinson KA, et al. Among authors: brown ja. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1621-5. doi: 10.1016/j.bmcl.2011.01.113. Epub 2011 Jan 31. Bioorg Med Chem Lett. 2011. PMID: 21324691
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: brown ja. 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 a Novel Small-Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis.
Menhaji-Klotz E, Hesp KD, Londregan AT, Kalgutkar AS, Piotrowski DW, Boehm M, Song K, Ryder T, Beaumont K, Jones RM, Atkinson K, Brown JA, Litchfield J, Xiao J, Canterbury DP, Burford K, Thuma BA, Limberakis C, Jiao W, Bagley SW, Agarwal S, Crowell D, Pazdziorko S, Ward J, Price DA, Clerin V. Menhaji-Klotz E, et al. Among authors: brown ja. J Med Chem. 2018 Apr 26;61(8):3685-3696. doi: 10.1021/acs.jmedchem.8b00190. Epub 2018 Apr 17. J Med Chem. 2018. PMID: 29627981
Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.
Cameron KO, Kung DW, Kalgutkar AS, Kurumbail RG, Miller R, Salatto CT, Ward J, Withka JM, Bhattacharya SK, Boehm M, Borzilleri KA, Brown JA, Calabrese M, Caspers NL, Cokorinos E, Conn EL, Dowling MS, Edmonds DJ, Eng H, Fernando DP, Frisbie R, Hepworth D, Landro J, Mao Y, Rajamohan F, Reyes AR, Rose CR, Ryder T, Shavnya A, Smith AC, Tu M, Wolford AC, Xiao J. Cameron KO, et al. Among authors: brown ja. J Med Chem. 2016 Sep 8;59(17):8068-81. doi: 10.1021/acs.jmedchem.6b00866. Epub 2016 Aug 20. J Med Chem. 2016. PMID: 27490827
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