2013 Publications

Boehm, M., Hepworth, D., Loria, P. M., Norquay, L. D., Filipski, K. J., Chin, J. E., Cameron, K. O., Brenner, M., Bonnette, P., Cabral, S., Ebner, D. C., Gautreau, D., Hadcock, J., Lee, E. C. Y., Mathiowetz, A., Morin, M., Rogers, L., Smith, A., VanVolkenburg, M., and Carpino, P. A. (2013) Chemical Probe Identification Platform for Orphan GPCRs Using Focused Compound Screening: GPR39 as a Case Example, ACS Med. Chem. Lett. 4, 1079-1084.

Breen, D. M., Rasmussen, B. A., Cote, C. D., Jackson, V. M., and Lam, T. K. (2013) Nutrient-sensing mechanisms in the gut as therapeutic targets for diabetes, Diabetes 62, 3005-3013.

Charest-Morin, X., Fortin, J. P., Bawolak, M. T., Lodge, R., and Marceau, F. (2013) Green fluorescent protein fused to peptide agonists of two dissimilar G protein coupled receptors: novel ligands of the bradykinin B2 (rhodopsin family) receptor and parathyroid hormone PTH1 (secretin family) receptor, Pharmacol. Res. Persp., 1-13.

Dow, R. L., Andrews, M. P., Li, J. C., Michael Gibbs, E., Guzman-Perez, A., Laperle, J. L., Li, Q., Mather, D., Munchhof, M. J., Niosi, M., Patel, L., Perreault, C., Tapley, S., and Zavadoski, W. J. (2013) Defining the key pharmacophore elements of PF-04620110: discovery of a potent, orally-active, neutral DGAT-1 inhibitor, Bioorg Med Chem 21, 5081-5097.

Eng, H., Sharma, R., McDonald, T. S., Edmonds, D. J., Fortin, J. P., Li, X., Stevens, B. D., Griffith, D. A., Limberakis, C., Nolte, W. M., Price, D. A., Jackson, M., and Kalgutkar, A. S. (2013) Demonstration of the innate electrophilicity of 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine (BETP), a small-molecule positive allosteric modulator of the glucagon-like peptide-1 receptor, Drug Metab Dispos 41, 1470-1479.

Filipski, K. J., Guzman-Perez, A., Bian, J., Perreault, C., Aspnes, G. E., Didiuk, M. T., Dow, R. L., Hank, R. F., Jones, C. S., Maguire, R. J., Tu, M., Zeng, D., Liu, S., Knafels, J. D., Litchfield, J., Atkinson, K., Derksen, D. R., Bourbonais, F., Gajiwala, K. S., Hickey, M., Johnson, T. O., Humphries, P. S., and Pfefferkorn, J. A. (2013) Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif, Bioorg Med Chem Lett 23, 4571-4578.

Flannick, J., Beer, N. L., Bick, A. G., Agarwala, V., Molnes, J., Gupta, N., Burtt, N. P., Florez, J. C., Meigs, J. B., Taylor, H., Lyssenko, V., Irgens, H., Fox, E., Burslem, F., Johansson, S., Brosnan, M. J., Trimmer, J. K., Newton-Cheh, C., Tuomi, T., Molven, A., Wilson, J. G., O'Donnell, C. J., Kathiresan, S., Hirschhorn, J. N., Njolstad, P. R., Rolph, T., Seidman, J. G., Gabriel, S., Cox, D. R., Seidman, C. E., Groop, L., and Altshuler, D. (2013) Assessing the phenotypic effects in the general population of rare variants in genes for a dominant Mendelian form of diabetes, Nat Genet 45, 1380-1385.

Griffith, D. A., Dow, R. L., Huard, K., Edmonds, D. J., Bagley, S. W., Polivkova, J., Zeng, D., Garcia-Irizarry, C. N., Southers, J. A., Esler, W., Amor, P., Loomis, K., McPherson, K., Bahnck, K. B., Preville, C., Banks, T., Moore, D. E., Mathiowetz, A. M., Menhaji-Klotz, E., Smith, A. C., Doran, S. D., Beebe, D. A., and Dunn, M. F. (2013) Spirolactam-based acetyl-CoA carboxylase inhibitors: toward improved metabolic stability of a chromanone lead structure, J Med Chem 56, 7110-7119.

Guzman-Perez, A., Pfefferkorn, J. A., Lee, E. C., Stevens, B. D., Aspnes, G. E., Bian, J., Didiuk, M. T., Filipski, K. J., Moore, D., Perreault, C., Sammons, M. F., Tu, M., Brown, J., Atkinson, K., Litchfield, J., Tan, B., Samas, B., Zavadoski, W. J., Salatto, C. T., and Treadway, J. (2013) 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, Bioorg Med Chem Lett 23, 3051-3058.

Londregan, A. T., Piotrowski, D. W., Futatsugi, K., Warmus, J. S., Boehm, M., Carpino, P. A., Chin, J. E., Janssen, A. M., Roush, N. S., Buxton, J., and Hinchey, T. (2013) Discovery of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as potent agonists of TGR5 via sequential combinatorial libraries, Bioorg Med Chem Lett 23, 1407-1411.

Maciejewski, B. S., LaPerle, J. L., Chen, D., Ghosh, A., Zavadoski, W. J., McDonald, T. S., Manion, T. B., Mather, D., Patterson, T. A., Hanna, M., Watkins, S., Gibbs, E. M., Calle, R. A., and Steppan, C. M. (2013) Pharmacological inhibition to examine the role of DGAT1 in dietary lipid absorption in rodents and humans, Am J Physiol Gastrointest Liver Physiol 304, G958-969.

McClure, K. F., Jackson, M., Cameron, K. O., Kung, D. W., Perry, D. A., Orr, S. T., Zhang, Y., Kohrt, J., Tu, M., Gao, H., Fernando, D., Jones, R., Erasga, N., Wang, G., Polivkova, J., Jiao, W., Swartz, R., Ueno, H., Bhattacharya, S. K., Stock, I. A., Varma, S., Bagdasarian, V., Perez, S., Kelly-Sullivan, D., Wang, R., Kong, J., Cornelius, P., Michael, L., Lee, E., Janssen, A., Steyn, S. J., Lapham, K., and Goosen, T. (2013) Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor, Bioorg Med Chem Lett 23, 5410-5414.

Menni, C., Fauman, E., Erte, I., Perry, J. R., Kastenmuller, G., Shin, S. Y., Petersen, A. K., Hyde, C., Psatha, M., Ward, K. J., Yuan, W., Milburn, M., Palmer, C. N., Frayling, T. M., Trimmer, J., Bell, J. T., Gieger, C., Mohney, R. P., Brosnan, M. J., Suhre, K., Soranzo, N., and Spector, T. D. (2013) Biomarkers for type 2 diabetes and impaired fasting glucose using a nontargeted metabolomics approach, Diabetes 62, 4270-4276.

Miao, Z., Nucci, G., Amin, N., Sharma, R., Mascitti, V., Tugnait, M., Vaz, A. D., Callegari, E., and Kalgutkar, A. S. (2013) Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects, Drug Metab Dispos 41, 445-456.

Milligan, P. A., Brown, M. J., Marchant, B., Martin, S. W., van der Graaf, P. H., Benson, N., Nucci, G., Nichols, D. J., Boyd, R. A., Mandema, J. W., Krishnaswami, S., Zwillich, S., Gruben, D., Anziano, R. J., Stock, T. C., and Lalonde, R. L. (2013) Model-based drug development: a rational approach to efficiently accelerate drug development, Clin Pharmacol Ther 93, 502-514.

Nambiar, P. R., Palanisamy, G. S., Okerberg, C., Wolford, A., Walters, K., Buckbinder, L., and Reagan, W. J. (2013) Toxicities Associated with 1-month Treatment with Propylthiouracil (PTU) and Methimazole (MMI) in Male Rats, Toxicol. Pathol.

Perreault, M., Feng, G., Will, S., Gareski, T., Kubasiak, D., Marquette, K., Vugmeyster, Y., Unger, T. J., Jones, J., Qadri, A., Hahm, S., Sun, Y., Rohde, C. M., Zwijnenberg, R., Paulsen, J., and Gimeno, R. E. (2013) Activation of TrkB with TAM-163 results in opposite effects on body weight in rodents and non-human primates, PLoS One 8, e62616.

Pfefferkorn, J. A. (2013) Strategies for the design of hepatoselective glucokinase activators to treat type 2 diabetes, Expert Opin Drug Discov 8, 319-330.

Sharma, R., McDonald, T. S., Eng, H., Limberakis, C., Stevens, B. D., Patel, S., and Kalgutkar, A. S. (2013) In vitro metabolism of the glucagon-like peptide-1 (GLP-1)-derived metabolites GLP-1(9-36)amide and GLP-1(28-36)amide in mouse and human hepatocytes, Drug Metab Dispos 41, 2148-2157.

Tu, M., Mathiowetz, A. M., Pfefferkorn, J. A., Cameron, K. O., Dow, R. L., Litchfield, J., Di, L., Feng, B., and Liras, S. (2013) Medicinal chemistry design principles for liver targeting through OATP transporters, Curr Top Med Chem 13, 857-866.

Ward, J., Spath, S. N., Pabst, B., Carpino, P. A., Ruggeri, R. B., Xing, G., Speers, A. E., Cravatt, B. F., and Ahn, K. (2013) Mechanistic characterization of a 2-thioxanthine myeloperoxidase inhibitor and selectivity assessment utilizing click chemistry--activity-based protein profiling, Biochemistry 52, 9187-9201.

Wu, J., Puppala, D., Feng, X., Monetti, M., Lapworth, A. L., and Geoghegan, K. F. (2013) Chemoproteomic analysis of intertissue and interspecies isoform diversity of AMP-activated protein kinase (AMPK), J Biol Chem 288, 35904-35912.

Zhou, Y., and Rui, L. (2013) Leptin signaling and leptin resistance, Front Med 7, 207-222.