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Page 1
Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging.
Liang SH, Chen JM, Normandin MD, Chang JS, Chang GC, Taylor CK, Trapa P, Plummer MS, Para KS, Conn EL, Lopresti-Morrow L, Lanyon LF, Cook JM, Richter KE, Nolan CE, Schachter JB, Janat F, Che Y, Shanmugasundaram V, Lefker BA, Enerson BE, Livni E, Wang L, Guehl NJ, Patnaik D, Wagner FF, Perlis R, Holson EB, Haggarty SJ, El Fakhri G, Kurumbail RG, Vasdev N. Liang SH, et al. Among authors: kurumbail rg. Angew Chem Int Ed Engl. 2016 Aug 8;55(33):9601-5. doi: 10.1002/anie.201603797. Epub 2016 Jun 29. Angew Chem Int Ed Engl. 2016. PMID: 27355874 Free PMC article.
Structural Basis for Achieving GSK-3β Inhibition with High Potency, Selectivity, and Brain Exposure for Positron Emission Tomography Imaging and Drug Discovery.
Bernard-Gauthier V, Mossine AV, Knight A, Patnaik D, Zhao WN, Cheng C, Krishnan HS, Xuan LL, Chindavong PS, Reis SA, Chen JM, Shao X, Stauff J, Arteaga J, Sherman P, Salem N, Bonsall D, Amaral B, Varlow C, Wells L, Martarello L, Patel S, Liang SH, Kurumbail RG, Haggarty SJ, Scott PJH, Vasdev N. Bernard-Gauthier V, et al. Among authors: kurumbail rg. J Med Chem. 2019 Nov 14;62(21):9600-9617. doi: 10.1021/acs.jmedchem.9b01030. Epub 2019 Oct 21. J Med Chem. 2019. PMID: 31535859 Free PMC article.
Identification of type-II inhibitors using kinase structures.
Lovering F, McDonald J, Whitlock GA, Glossop PA, Phillips C, Bent A, Sabnis Y, Ryan M, Fitz L, Lee J, Chang JS, Han S, Kurumbail R, Thorarensen A. Lovering F, et al. Chem Biol Drug Des. 2012 Nov;80(5):657-64. doi: 10.1111/j.1747-0285.2012.01443.x. Epub 2012 Sep 3. Chem Biol Drug Des. 2012. PMID: 22759374
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: kurumbail rg. 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
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: kurumbail rg. 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
Rational approach to highly potent and selective apoptosis signal-regulating kinase 1 (ASK1) inhibitors.
Lovering F, Morgan P, Allais C, Aulabaugh A, Brodfuehrer J, Chang J, Coe J, Ding W, Dowty H, Fleming M, Frisbie R, Guzova J, Hepworth D, Jasti J, Kortum S, Kurumbail R, Mohan S, Papaioannou N, Strohbach JW, Vincent F, Lee K, Zapf CW. Lovering F, et al. Eur J Med Chem. 2018 Feb 10;145:606-621. doi: 10.1016/j.ejmech.2017.12.041. Epub 2017 Dec 15. Eur J Med Chem. 2018. PMID: 29348070
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: kurumbail rg. 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.
Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.
Henderson JL, Kormos BL, Hayward MM, Coffman KJ, Jasti J, Kurumbail RG, Wager TT, Verhoest PR, Noell GS, Chen Y, Needle E, Berger Z, Steyn SJ, Houle C, Hirst WD, Galatsis P. Henderson JL, et al. Among authors: kurumbail rg. J Med Chem. 2015 Jan 8;58(1):419-32. doi: 10.1021/jm5014055. Epub 2014 Nov 17. J Med Chem. 2015. PMID: 25353650
Selectively targeting an inactive conformation of interleukin-2-inducible T-cell kinase by allosteric inhibitors.
Han S, Czerwinski RM, Caspers NL, Limburg DC, Ding W, Wang H, Ohren JF, Rajamohan F, McLellan TJ, Unwalla R, Choi C, Parikh MD, Seth N, Edmonds J, Phillips C, Shakya S, Li X, Spaulding V, Hughes S, Cook A, Robinson C, Mathias JP, Navratilova I, Medley QG, Anderson DR, Kurumbail RG, Aulabaugh A. Han S, et al. Among authors: kurumbail rg. Biochem J. 2014 Jun 1;460(2):211-22. doi: 10.1042/BJ20131139. Biochem J. 2014. PMID: 24593284
62 results