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Page 1
Activation of Liver AMPK with PF-06409577 Corrects NAFLD and Lowers Cholesterol in Rodent and Primate Preclinical Models.
Esquejo RM, Salatto CT, Delmore J, Albuquerque B, Reyes A, Shi Y, Moccia R, Cokorinos E, Peloquin M, Monetti M, Barricklow J, Bollinger E, Smith BK, Day EA, Nguyen C, Geoghegan KF, Kreeger JM, Opsahl A, Ward J, Kalgutkar AS, Tess D, Butler L, Shirai N, Osborne TF, Steinberg GR, Birnbaum MJ, Cameron KO, Miller RA. Esquejo RM, et al. Among authors: kalgutkar as. EBioMedicine. 2018 May;31:122-132. doi: 10.1016/j.ebiom.2018.04.009. Epub 2018 Apr 8. EBioMedicine. 2018. PMID: 29673898 Free PMC article.
Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism.
Ahn K, Boehm M, Brown MF, Calloway J, Che Y, Chen J, Fennell KF, Geoghegan KF, Gilbert AM, Gutierrez JA, Kalgutkar AS, Lanba A, Limberakis C, Magee TV, O'Doherty I, Oliver R, Pabst B, Pandit J, Parris K, Pfefferkorn JA, Rolph TP, Patel R, Schuff B, Shanmugasundaram V, Starr JT, Varghese AH, Vera NB, Vernochet C, Yan J. Ahn K, et al. Among authors: kalgutkar as. ACS Chem Biol. 2016 Sep 16;11(9):2529-40. doi: 10.1021/acschembio.6b00266. Epub 2016 Jul 19. ACS Chem Biol. 2016. PMID: 27391855
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: kalgutkar as. 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: kalgutkar as. 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
Activation of Skeletal Muscle AMPK Promotes Glucose Disposal and Glucose Lowering in Non-human Primates and Mice.
Cokorinos EC, Delmore J, Reyes AR, Albuquerque B, Kjøbsted R, Jørgensen NO, Tran JL, Jatkar A, Cialdea K, Esquejo RM, Meissen J, Calabrese MF, Cordes J, Moccia R, Tess D, Salatto CT, Coskran TM, Opsahl AC, Flynn D, Blatnik M, Li W, Kindt E, Foretz M, Viollet B, Ward J, Kurumbail RG, Kalgutkar AS, Wojtaszewski JFP, Cameron KO, Miller RA. Cokorinos EC, et al. Among authors: kalgutkar as. Cell Metab. 2017 May 2;25(5):1147-1159.e10. doi: 10.1016/j.cmet.2017.04.010. Cell Metab. 2017. PMID: 28467931 Free article.
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: kalgutkar as. 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
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: kalgutkar as. 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
Myeloperoxidase inhibition in mice alters atherosclerotic lesion composition.
Roth Flach RJ, Su C, Bollinger E, Cortes C, Robertson AW, Opsahl AC, Coskran TM, Maresca KP, Keliher EJ, Yates PD, Kim AM, Kalgutkar AS, Buckbinder L. Roth Flach RJ, et al. Among authors: kalgutkar as. PLoS One. 2019 Mar 19;14(3):e0214150. doi: 10.1371/journal.pone.0214150. eCollection 2019. PLoS One. 2019. PMID: 30889221 Free PMC article.
Structural attributes influencing unbound tissue distribution.
Orozco CC, Atkinson K, Ryu S, Chang G, Keefer C, Lin J, Riccardi K, Mongillo RK, Tess D, Filipski KJ, Kalgutkar AS, Litchfield J, Scott D, Di L. Orozco CC, et al. Among authors: kalgutkar as. Eur J Med Chem. 2020 Jan 1;185:111813. doi: 10.1016/j.ejmech.2019.111813. Epub 2019 Oct 28. Eur J Med Chem. 2020. PMID: 31732255
174 results