2012 Publications

Bagley, S. W., Southers, J. A., Cabral, S., Rose, C. R., Bernhardson, D. J., Edmonds, D. J., Polivkova, J., Yang, X., Kung, D. W., Griffith, D. A., and Bader, S. J. (2012) Synthesis of 7-oxo-dihydrospiro[indazole-5,4'-piperidine] acetyl-CoA carboxylase inhibitors, J Org Chem 77, 1497-1506.

Bhattacharya, S. K., Aspnes, G. E., Bagley, S. W., Boehm, M., Brosius, A. D., Buckbinder, L., Chang, J. S., Dibrino, J., Eng, H., Frederick, K. S., Griffith, D. A., Griffor, M. C., Guimaraes, C. R., Guzman-Perez, A., Han, S., Kalgutkar, A. S., Klug-McLeod, J., Garcia-Irizarry, C., Li, J., Lippa, B., Price, D. A., Southers, J. A., Walker, D. P., Wei, L., Xiao, J., Zawistoski, M. P., and Zhao, X. (2012) Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors, Bioorg Med Chem Lett 22, 7523-7529.

Bourbonais, F. J., Chen, J., Huang, C., Zhang, Y., Pfefferkorn, J. A., and Landro, J. A. (2012) Modulation of glucokinase by glucose, small-molecule activator and glucokinase regulatory protein: steady-state kinetic and cell-based analysis, Biochem J 441, 881-887.

Cameron, K. O., Beretta, E. E., Chen, Y., Chu-Moyer, M., Fernando, D., Gao, H., Kohrt, J., Lavergne, S., Jardine Pda, S., Guzman-Perez, A., Hoth, C., Perry, D. A., Hadcock, J. R., Gautreau, D., Makowski, M., Perez, S., Polivkova, J., Rogers, L., Scott, D. O., Swick, A. G., Thiede, L., Trebino, C. E., Trilles, R. V., Wilmowski, J., and Zhang, Y. (2012) Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists, Bioorg Med Chem Lett 22, 2943-2947.

Carpino, P. A., and Hepworth, D. (2012) Beyond PPARs and Metformin: New Insulin Sensitizers for the Treatment of Type 2 Diabetes, Ann Rep Med Chem 47, 177–192.

DeNinno, M. P., Wright, S. W., Etienne, J. B., Olson, T. V., Rocke, B. N., Corbett, J. W., Kung, D. W., DiRico, K. J., Andrews, K. M., Millham, M. L., Parker, J. C., Esler, W., van Volkenburg, M., Boyer, D. D., Houseknecht, K. L., and Doran, S. D. (2012) Discovery of triazolopyrimidine-based PDE8B inhibitors: exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes, Bioorg Med Chem Lett 22, 5721-5726.

Deshmukh, H. A., Colhoun, H. M., Johnson, T., McKeigue, P. M., Betteridge, D. J., Durrington, P. N., Fuller, J. H., Livingstone, S., Charlton-Menys, V., Neil, A., Poulter, N., Sever, P., Shields, D. C., Stanton, A. V., Chatterjee, A., Hyde, C., Calle, R. A., Demicco, D. A., Trompet, S., Postmus, I., Ford, I., Jukema, J. W., Caulfield, M., and Hitman, G. A. (2012) Genome-wide association study of genetic determinants of LDL-c response to atorvastatin therapy: Importance of Lp(a), J Lipid Res 53, 1000-1011.

Dow, R. L. (2012) New Therapeutic Strategies for Type 2 Diabetes: Small Molecule Approaches; Acyl-CoA: Diacylglycerol Acyltransferase-1 Inhibition as an Approach to the Treatment of Type 2 Diabetes, pp 215-248, RSC Publishing, Cambridge, UK.

Dow, R. L., Carpino, P. A., Gautreau, D., Hadcock, J. R., Iredale, P. A., Kelly-Sullivan, D., Lizano, J. S., O'Connor, R. E., Schneider, S. R., Scott, D. O., and Ward, K. M. (2012) Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents, ACS Medicinal Chemistry Letters 3, 397-401.

Fichtner, M., Lee, E., Tomlinson, E., Scott, D., Cornelius, P., Patterson, T. A., and Carpino, P. A. (2012) Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor, Bioorg Med Chem Lett 22, 2738-2743.

Filipski, K. J., Bian, J., Ebner, D. C., Lee, E. C., Li, J. C., Sammons, M. F., Wright, S. W., Stevens, B. D., Didiuk, M. T., Tu, M., Perreault, C., Brown, J., Atkinson, K., Tan, B., Salatto, C. T., Litchfield, J., Pfefferkorn, J. A., and Guzman-Perez, A. (2012) A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity, Bioorg Med Chem Lett 22, 415-420.

Filipski, K.J., Futatsugi, K., Pfefferkorn, J. A., and Stevens, B.D. (2012) Glucokinase Activators, Pharm. Pat. Analyst, 1(3), 301-311.

Filipski, K.J., Stevens, B.D., and Pfefferkorn, J.A. (2012) New Therapeutic Strategies for Type 2 Diabetes: Small Molecule Approaches; Glucokinase Activators in Development, pp 88-108, RSC Publishing, Cambridge, UK.

Freeman-Cook, K. D., Amor, P., Bader, S., Buzon, L. M., Coffey, S. B., Corbett, J. W., Dirico, K. J., Doran, S. D., Elliott, R. L., Esler, W., Guzman-Perez, A., Henegar, K. E., Houser, J. A., Jones, C. S., Limberakis, C., Loomis, K., McPherson, K., Murdande, S., Nelson, K. L., Phillion, D., Pierce, B. S., Song, W., Sugarman, E., Tapley, S., Tu, M., and Zhao, Z. (2012) Maximizing lipophilic efficiency: the use of Free-Wilson analysis in the design of inhibitors of acetyl-CoA carboxylase, J Med Chem 55, 935-942.

Futatsugi, K., Mascitti, V., Guimaraes, C. R., Morishita, N., Cai, C., Deninno, M. P., Gao, H., Hamilton, M. D., Hank, R., Harris, A. R., Kung, D. W., Lavergne, S. Y., Lefker, B. A., Lopaze, M. G., McClure, K. F., Munchhof, M. J., Preville, C., Robinson, R. P., Wright, S. W., Bonin, P. D., Cornelius, P., Chen, Y., and Kalgutkar, A. S. (2012) From partial to full agonism: Identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor, Bioorg Med Chem Lett, In Press

Geoghegan, K. F., Varghese, A. H., Feng, X., Bessire, A. J., Conboy, J. J., Ruggeri, R. B., Ahn, K., Spath, S. N., Filippov, S. V., Conrad, S. J., Carpino, P. A., Guimaraes, C. R., and Vajdos, F. F. (2012) Deconstruction of Activity-Dependent Covalent Modification of Heme in Human Neutrophil Myeloperoxidase by Multistage Mass Spectrometry (MS(4)), Biochemistry 51, 2065-2077.

Hall, A. M., Kou, K., Chen, Z., Pietka, T. A., Kumar, M., Korenblat, K. M., Lee, K., Ahn, K., Fabbrini, E., Klein, S., Goodwin, B., and Finck, B. N. (2012) Evidence for regulated monoacylglycerol acyltransferase expression and activity in human liver, J Lipid Res 53, 990-999.

Kung, D. W., Coffey, S. B., Jones, R. M., Cabral, S., Jiao, W., Fichtner, M., Carpino, P. A., Rose, C. R., Hank, R. F., Lopaze, M. G., Swartz, R., Chen, H. T., Hendsch, Z., Posner, B., Wielis, C. F., Manning, B., Dubins, J., Stock, I. A., Varma, S., Campbell, M., DeBartola, D., Kosa-Maines, R., Steyn, S. J., and McClure, K. F. (2012) Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor, Bioorg Med Chem Lett 22, 4281-4287.

Liu, S., Ammirati, M. J., Song, X., Knafels, J. D., Zhang, J., Greasley, S. E., Pfefferkorn, J. A., and Qiu, X. (2012) Insights into the mechanism of glucokinase activation: observation of multiple distinct protein conformations, J Biol Chem 287, 13598-13610.

Liu, S., Mistry, A., Reynolds, J. M., Lloyd, D. B., Griffor, M. C., Perry, D. A., Ruggeri, R. B., Clark, R. W., and Qiu, X. (2012) Crystal structures of cholesteryl ester transfer protein in complex with inhibitors, J Biol Chem 287, 37321-37329.

Mamidyala, S. K., Dutta, S., Chrunyk, B. A., Preville, C., Wang, H., Withka, J. M., McColl, A., Subashi, T. A., Hawrylik, S. J., Griffor, M. C., Kim, S., Pfefferkorn, J. A., Price, D. A., Menhaji-Klotz, E., Mascitti, V., and Finn, M. G. (2012) Glycomimetic ligands for the human asialoglycoprotein receptor, J Am Chem Soc 134, 1978-1981.

Normandin, M. D., Petersen, K. F., Ding, Y. S., Lin, S. F., Naik, S., Fowles, K., Skovronsky, D. M., Herold, K. C., McCarthy, T. J., Calle, R. A., Carson, R. E., Treadway, J. L., and Cline, G. W. (2012) In vivo imaging of endogenous pancreatic beta-cell mass in healthy and type 1 diabetic subjects using 18F-fluoropropyl-dihydrotetrabenazine and PET, J Nucl Med 53, 908-916.

Pfefferkorn, J. A., Guzman-Perez, A., Litchfield, J., Aiello, R., Treadway, J. L., Pettersen, J., Minich, M. L., Filipski, K. J., Jones, C. S., Tu, M., Aspnes, G., Risley, H., Bian, J., Stevens, B. D., Bourassa, P., D'Aquila, T., Baker, L., Barucci, N., Robertson, A. S., Bourbonais, F., Derksen, D. R., Macdougall, M., Cabrera, O., Chen, J., Lapworth, A. L., Landro, J. A., Zavadoski, W. J., Atkinson, K., Haddish-Berhane, N., Tan, B., Yao, L., Kosa, R. E., Varma, M. V., Feng, B., Duignan, D. B., El-Kattan, A., Murdande, S., Liu, S., Ammirati, M., Knafels, J., Dasilva-Jardine, P., Sweet, L., Liras, S., and Rolph, T. P. (2012) Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotini c acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus, J Med Chem 55, 1318-1333.

Pfefferkorn, J. A., Tu, M., Filipski, K. J., Guzman-Perez, A., Bian, J., Aspnes, G. E., Sammons, M. F., Song, W., Li, J. C., Jones, C. S., Patel, L., Rasmusson, T., Zeng, D., Karki, K., Hamilton, M., Hank, R., Atkinson, K., Litchfield, J., Aiello, R., Baker, L., Barucci, N., Bourassa, P., Bourbounais, F., D'Aquila, T., Derksen, D. R., Macdougall, M., and Robertson, A. (2012) The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus, Bioorg Med Chem Lett 22, 7100-7105.

Powell, N. A., Kohrt, J. T., Filipski, K. J., Kaufman, M., Sheehan, D., Edmunds, J. E., Delaney, A., Wang, Y., Bourbonais, F., Lee, D. Y., Schwende, F., Sun, F., McConnell, P., Catana, C., Chen, H., Ohren, J., and Perrin, L. A. (2012) Novel and selective spiroindoline-based inhibitors of Sky kinase, Bioorg Med Chem Lett 22, 190-193.

Ruangsiriluk, W., Grosskurth, S. E., Ziemek, D., Kuhn, M., des Etages, S. G., and Francone, O. L. (2012) Silencing of enzymes involved in ceramide biosynthesis causes distinct global alterations of lipid homeostasis and gene expression, J Lipid Res 53, 1459-1471.

Schmidt, B. J., Papin, J. A., and Musante, C. J. (2012) Mechanistic systems modeling to guide drug discovery and development, Drug Discov Today.

Skaddan, M. B., Zhang, L., Johnson, D. S., Zhu, A., Zasadny, K. R., Coelho, R. V., Kuszpit, K., Currier, G., Fan, K. H., Beck, E. M., Chen, L., Drozda, S. E., Balan, G., Niphakis, M., Cravatt, B. F., Ahn, K., Bocan, T., and Villalobos, A. (2012) The synthesis and in vivo evaluation of [18F]PF-9811: a novel PET ligand for imaging brain fatty acid amide hydrolase (FAAH), Nucl Med Biol 39, 1058-1067.

Stanton, R., Sciabola, S., Salatto, C., Weng, Y., Moshinsky, D., Little, J., Walters, E., Kreeger, J., DiMattia, D., Chen, T., Clark, T., Liu, M., Qian, J., Roy, M., and Dullea, R. (2012) Chemical modification study of antisense gapmers, Nucleic Acid Ther 22, 344-359.

Talukdar, S., Oh da, Y., Bandyopadhyay, G., Li, D., Xu, J., McNelis, J., Lu, M., Li, P., Yan, Q., Zhu, Y., Ofrecio, J., Lin, M., Brenner, M. B., and Olefsky, J. M. (2012) Neutrophils mediate insulin resistance in mice fed a high-fat diet through secreted elastase, Nat Med 18, 1407-1412.

Tremblay, F., Huard, C., Dow, J., Gareski, T., Will, S., Richard, A. M., Syed, J., Bailey, S., Brenneman, K. A., Martinez, R. V., Perreault, M., Lin, Q., and Gimeno, R. E. (2012) Loss of coiled-coil domain containing 80 negatively modulates glucose homeostasis in diet-induced obese mice, Endocrinology 153, 4290-4303.

Tse, K. W., Lin, K. B., Dang-Lawson, M., Guzman-Perez, A., Aspnes, G. E., Buckbinder, L., and Gold, M. R. (2012) Small molecule inhibitors of the Pyk2 and FAK kinases modulate chemoattractant-induced migration, adhesion and Akt activation in follicular and marginal zone B cells, Cell Immunol 275, 47-54.

Tu, M., Rai, B. K., Mathiowetz, A. M., Didiuk, M., Pfefferkorn, J. A., Guzman-Perez, A., Benbow, J., Guimaraes, C. R., Mente, S., Hayward, M. M., and Liras, S. (2012) Exploring aromatic chemical space with NEAT: novel and electronically equivalent aromatic template, J Chem Inf Model 52, 1114-1123.

van Leeuwen, N., Nijpels, G., Becker, M. L., Deshmukh, H., Zhou, K., Stricker, B. H., Uitterlinden, A. G., Hofman, A., van 't Riet, E., Palmer, C. N., Guigas, B., Slagboom, P. E., Durrington, P., Calle, R. A., Neil, A., Hitman, G., Livingstone, S. J., Colhoun, H., Holman, R. R., McCarthy, M. I., Dekker, J. M., t Hart, L. M., and Pearson, E. R. (2012) A gene variant near ATM is significantly associated with metformin treatment response in type 2 diabetes: a replication and meta-analysis of five cohorts, Diabetologia 55, 1971-1977.

Wang, M., Defranco, D., Wright, K., Quazi, S., Chen, J., Spencer-Pierce, J., Zaghloul, I., Pak, R., Darvair, R., Krishnan, A., Perreault, M., Sun, L., Ozer, J., and Xu, X. (2012) Decreased Subcutaneous Bioavailability of an Oxyntomodulin Analog in a Controlled Release Formulation Could Be Caused by Skin Metabolism in Rats, J Bioequival & Bioavail 4, 69-77.