2011 Publications

Abraham, A. K., Maurer, T. S., Kalgutkar, A. S., Gao, X., Li, M., Healy, D. R., Petersen, D. N., Griffith, D. A., and Mager, D. E. (2011) Pharmacodynamic model of parathyroid hormone modulation by a negative allosteric modulator of the calcium-sensing receptor, AAPS J 13, 265-273.

Ahn, K., Smith, S. E., Liimatta, M. B., Beidler, D., Sadagopan, N., Dudley, D. T., Young, T., Wren, P., Zhang, Y., Swaney, S., Van Becelaere, K., Blankman, J. L., Nomura, D. K., Bhattachar, S. N., Stiff, C., Nomanbhoy, T. K., Weerapana, E., Johnson, D. S., and Cravatt, B. F. (2011) Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain, J Pharmacol Exp Ther 338, 114-124.

Atkinson, K. A., Beretta, E. E., Brown, J. A., Castrodad, M., Chen, Y., Cosgrove, J. M., Du, P., Litchfield, J., Makowski, M., Martin, K., McLellan, T. J., Neagu, C., Perry, D. A., Piotrowski, D. W., Steppan, C. M., and Trilles, R. (2011) N-benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors, Bioorg Med Chem Lett 21, 1621-1625.

Boustany-Kari, C. M., Jackson, V. M., Gibbons, C. P., and Swick, A. G. (2011) Leptin potentiates the anti-obesity effects of rimonabant, Eur J Pharmacol 658, 270-276.

Cao, J., Zhou, Y., Peng, H., Huang, X., Stahler, S., Suri, V., Qadri, A., Gareski, T., Jones, J., Hahm, S., Perreault, M., McKew, J., Shi, M., Xu, X., Tobin, J. F., and Gimeno, R. E. (2011) Targeting Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases, J Biol Chem 286, 41838-41851.

Dow, R. L., Andrews, M., Aspnes, G. E., Balan, G., Michael Gibbs, E., Guzman-Perez, A., Karki, K., Laperle, J. L., Li, J. C., Litchfield, J., Munchhof, M. J., Perreault, C., and Patel, L. (2011) Design and synthesis of potent, orally-active DGAT-1 inhibitors containing a dioxino[2,3-d]pyrimidine core, Bioorg Med Chem Lett 21, 6122-6125.

Enayetallah, A. E., Ziemek, D., Leininger, M. T., Randhawa, R., Yang, J., Manion, T. B., Mather, D. E., Zavadoski, W. J., Kuhn, M., Treadway, J. L., des Etages, S. A., Gibbs, E. M., Greene, N., and Steppan, C. M. (2011) Modeling the mechanism of action of a DGAT1 inhibitor using a causal reasoning platform, PLoS One 6, e27009.

Griffith, D. A., Hargrove, D. M., Maurer, T. S., Blum, C. A., De Lombaert, S., Inthavongsay, J. K., Klade, L. E., Mack, C. M., Rose, C. R., Sanders, M. J., and Carpino, P. A. (2011) Discovery and evaluation of pyrazolo[1,5-a]pyrimidines as neuropeptide Y1 receptor antagonists, Bioorg Med Chem Lett 21, 2641-2645.

Guimaraes, C. R., Rai, B. K., Munchhof, M. J., Liu, S., Wang, J., Bhattacharya, S. K., and Buckbinder, L. (2011) Understanding the Impact of the P-loop Conformation on Kinase Selectivity, J Chem Inf Model 51, 1199-1204.

Gustavson, S. M., Chen, D., Somayaji, V., Hudson, K., Baltrukonis, D. J., Singh, J., Boyden, T. L., and Calle, R. A. (2011) Effects of a long-acting GLP-1 mimetic (PF-04603629) on pulse rate and diastolic blood pressure in patients with type 2 diabetes mellitus, Diabetes Obes Metab 13, 1056-1058.

Gustavson, S. M., Dai, H., Preston, G. M., Somayaji, V., Hirshberg, B., and Calle, R. A. (2011) Effects of multiple doses of the DPP-IV inhibitor PF-734200 on the relationship between GLP-1 and glucose in subjects with type 2 diabetes mellitus, Diabetes Res Clin Pract 91, e45-49.

Johnson, D. S., Stiff, C., Lazerwith, S. E., Kesten, S. R., Fay, L. K., Morris, M., Beidler, D., Liimatta, M. B., Smith, S. E., Dudley, D. T., Sadagopan, N., Bhattachar, S. N., Kesten, S. J., Nomanbhoy, T. K., Cravatt, B. F., and Ahn, K. (2011) Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor, ACS Med Chem Lett 2, 91-96.

Mascitti, V., Maurer, T. S., Robinson, R. P., Bian, J., Boustany-Kari, C. M., Brandt, T., Collman, B. M., Kalgutkar, A. S., Klenotic, M. K., Leininger, M. T., Lowe, A., Maguire, R. J., Masterson, V. M., Miao, Z., Mukaiyama, E., Patel, J. D., Pettersen, J. C., Preville, C., Samas, B., She, L., Sobol, Z., Steppan, C. M., Stevens, B. D., Thuma, B. A., Tugnait, M., Zeng, D., and Zhu, T. (2011) Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors, J Med Chem 54, 2952-2960.

McClure, K. F., Darout, E., Guimaraes, C. R., DeNinno, M. P., Mascitti, V., Munchhof, M. J., Robinson, R. P., Kohrt, J., Harris, A. R., Moore, D. E., Li, B., Samp, L., Lefker, B. A., Futatsugi, K., Kung, D., Bonin, P. D., Cornelius, P., Wang, R., Salter, E., Hornby, S., Kalgutkar, A. S., and Chen, Y. (2011) Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response, J Med Chem 54, 1948-1952.

Pfefferkorn, J. A. (2011) Novel 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors: a patent review, Expert Opin Ther Pat 21, 187-203.

Pfefferkorn, J. A., Guzman-Perez, A., Oates, P. J., Litchfield, J., Aspnes, G., Basak, A., Benbow, J., Berliner, M. A., Bian, J., Choi, C., Freeman-Cook, K., Corbett, J. W., Didiuk, M., Dunetz, J. R., Filipski, K. J., Hungerford, W. M., Jones, C. S., Karki, K., Ling, A., Li, J. C., Patel, L., Risley, H., Saenz, J., Song, W., Tu, T., Aiello, R., Atkinson, K., Barucci, N., Beebe, D., Bourassa, P., Bourbounais, F., Brodeur, A. M., Burbey, R., Chen, J., D’Aquila, T., Derksen, D. R., Haddish-Berhane, N., Huang, C., Landro, J., Lapworth, A. L., MacDougall, M., Perregaux, D., Pettersen, J., Robertson, A., Tan, B., Treadway, J. L., Liu, S., Qiu, X., Knafels, J., Ammirati, M., Song, X., DaSilva-Jardine, P., Liras, S., Sweet, L., and Rolph, T. P. (2011) Designing Glucokinase Activators with Reduced Hypoglycemia Risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a Clinical Candidate for the Treatment of Type 2 Diabetes Mellitus, Med Chem Comm 2, 828-839.

Pfefferkorn, J. A., Litchfield, J., Hutchings, R., Cheng, X. M., Larsen, S. D., Auerbach, B., Bush, M. R., Lee, C., Erasga, N., Bowles, D. M., Boyles, D. C., Lu, G., Sekerke, C., Askew, V., Hanselman, J. C., Dillon, L., Lin, Z., Robertson, A., Olsen, K., Boustany, C., Atkinson, K., Goosen, T. C., Sahasrabudhe, V., Chupka, J., Duignan, D. B., Feng, B., Scialis, R., Kimoto, E., Bi, Y. A., Lai, Y., El-Kattan, A., Bakker-Arkema, R., Barclay, P., Kindt, E., Le, V., Mandema, J. W., Milad, M., Tait, B. D., Kennedy, R., Trivedi, B. K., and Kowala, M. (2011) Discovery of novel hepatoselective HMG-CoA reductase inhibitors for treating hypercholesterolemia: a bench-to-bedside case study on tissue selective drug distribution, Bioorg Med Chem Lett 21, 2725-2731.

Shen, C. J., Raghavan, S., Xu, Z., Baranski, J. D., Yu, X., Wozniak, M. A., Miller, J. S., Gupta, M., Buckbinder, L., and Chen, C. S. (2011) Decreased cell adhesion promotes angiogenesis in a Pyk2-dependent manner, Exp Cell Res 317, 1860-1871.

Skepner, J. E., Shelly, L. D., Ji, C., Reidich, B., and Luo, Y. (2011) Chronic treatment with epoxyeicosatrienoic acids modulates insulin signaling and prevents insulin resistance in hepatocytes, Prostaglandins Other Lipid Mediators 94, 3-8.

Straub, S. V., Perez, S. M., Tan, B., Coughlan, K. A., Trebino, C. E., Cosgrove, P., Buxton, J. M., Kreeger, J. M., and Jackson, V. M. (2011) Pharmacological inhibition of Kv1.3 fails to modulate insulin sensitivity in diabetic mice or human insulin-sensitive tissues, Am J Physiol Endocrinol Metab, E380-390

Terra, S. G., Somayaji, V., Schwartz, S., Lewin, A. J., Teeter, J. G., Dai, H., Nguyen, T. T., and Calle, R. A. (2011) A Dose-Ranging Study of the DPP-IV Inhibitor PF-734200 Added to Metformin in Subjects With Type 2 Diabetes*, Exp Clin Endocrinol Diabetes 119, 401-407.

Xing, Y., Cohen, A., Rothblat, G., Sankaranarayanan, S., Weibel, G., Royer, L., Francone, O. L., and Rainey, W. E. (2011) Aldosterone production in human adrenocortical cells is stimulated by high-density lipoprotein 2 (HDL2) through increased expression of aldosterone synthase (CYP11B2), Endocrinology 152, 751-763.