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Page 1
Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK).
Ryder TF, Calabrese MF, Walker GS, Cameron KO, Reyes AR, Borzilleri KA, Delmore J, Miller R, Kurumbail RG, Ward J, Kung DW, Brown JA, Edmonds DJ, Eng H, Wolford AC, Kalgutkar AS. Ryder TF, et al. Among authors: ward j. J Med Chem. 2018 Aug 23;61(16):7273-7288. doi: 10.1021/acs.jmedchem.8b00807. Epub 2018 Aug 2. J Med Chem. 2018. PMID: 30036059
SRT1720, SRT2183, SRT1460, and resveratrol are not direct activators of SIRT1.
Pacholec M, Bleasdale JE, Chrunyk B, Cunningham D, Flynn D, Garofalo RS, Griffith D, Griffor M, Loulakis P, Pabst B, Qiu X, Stockman B, Thanabal V, Varghese A, Ward J, Withka J, Ahn K. Pacholec M, et al. Among authors: ward j. J Biol Chem. 2010 Mar 12;285(11):8340-51. doi: 10.1074/jbc.M109.088682. Epub 2010 Jan 8. J Biol Chem. 2010. PMID: 20061378 Free PMC article.
Structural basis for AMPK activation: natural and synthetic ligands regulate kinase activity from opposite poles by different molecular mechanisms.
Calabrese MF, Rajamohan F, Harris MS, Caspers NL, Magyar R, Withka JM, Wang H, Borzilleri KA, Sahasrabudhe PV, Hoth LR, Geoghegan KF, Han S, Brown J, Subashi TA, Reyes AR, Frisbie RK, Ward J, Miller RA, Landro JA, Londregan AT, Carpino PA, Cabral S, Smith AC, Conn EL, Cameron KO, Qiu X, Kurumbail RG. Calabrese MF, et al. Among authors: ward j. Structure. 2014 Aug 5;22(8):1161-1172. doi: 10.1016/j.str.2014.06.009. Epub 2014 Jul 24. Structure. 2014. PMID: 25066137 Free article.
PF-1355, a mechanism-based myeloperoxidase inhibitor, prevents immune complex vasculitis and anti-glomerular basement membrane glomerulonephritis.
Zheng W, Warner R, Ruggeri R, Su C, Cortes C, Skoura A, Ward J, Ahn K, Kalgutkar A, Sun D, Maurer TS, Bonin PD, Okerberg C, Bobrowski W, Kawabe T, Zhang Y, Coskran T, Bell S, Kapoor B, Johnson K, Buckbinder L. Zheng W, et al. Among authors: ward j. J Pharmacol Exp Ther. 2015 May;353(2):288-98. doi: 10.1124/jpet.114.221788. Epub 2015 Feb 19. J Pharmacol Exp Ther. 2015. PMID: 25698787
Probing the enzyme kinetics, allosteric modulation and activation of α1- and α2-subunit-containing AMP-activated protein kinase (AMPK) heterotrimeric complexes by pharmacological and physiological activators.
Rajamohan F, Reyes AR, Frisbie RK, Hoth LR, Sahasrabudhe P, Magyar R, Landro JA, Withka JM, Caspers NL, Calabrese MF, Ward J, Kurumbail RG. Rajamohan F, et al. Among authors: ward j. Biochem J. 2016 Mar 1;473(5):581-92. doi: 10.1042/BJ20151051. Epub 2015 Dec 3. Biochem J. 2016. PMID: 26635351 Free PMC article.
Development of a selective activity-based probe for glycosylated LIPA.
Schwaid AG, Ruangsiriluk W, Reyes AR, Cabral S, Rajamohan F, Tu M, Ward J, Carpino PA. Schwaid AG, et al. Among authors: ward j. Bioorg Med Chem Lett. 2016 Apr 15;26(8):1993-6. doi: 10.1016/j.bmcl.2016.02.089. Epub 2016 Mar 2. Bioorg Med Chem Lett. 2016. PMID: 26965858
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: ward j. 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
Selective Activation of AMPK β1-Containing Isoforms Improves Kidney Function in a Rat Model of Diabetic Nephropathy.
Salatto CT, Miller RA, Cameron KO, Cokorinos E, Reyes A, Ward J, Calabrese MF, Kurumbail RG, Rajamohan F, Kalgutkar AS, Tess DA, Shavnya A, Genung NE, Edmonds DJ, Jatkar A, Maciejewski BS, Amaro M, Gandhok H, Monetti M, Cialdea K, Bollinger E, Kreeger JM, Coskran TM, Opsahl AC, Boucher GG, Birnbaum MJ, DaSilva-Jardine P, Rolph T. Salatto CT, et al. Among authors: ward j. J Pharmacol Exp Ther. 2017 May;361(2):303-311. doi: 10.1124/jpet.116.237925. Epub 2017 Mar 13. J Pharmacol Exp Ther. 2017. PMID: 28289077
6,260 results