Search Results - "Shaffer, Alexander F."

Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation by Arhancet, Graciela B., Walker, Daniel P., Metz, Sue, Fobian, Yvette M., Heasley, Steven E., Carter, Jeffrey S., Springer, John R., Jones, Darin E., Hayes, Michael J., Shaffer, Alexander F., Jerome, Gina M., Baratta, Michael T., Zweifel, Ben, Moore, William M., Masferrer, Jaime L., Vazquez, Michael L.

“…Inhibition of mPGES-1, the terminal enzyme in the arachidonic acid/COX pathway to regulate the production of pro-inflammatory prostaglandin PGE2, is considered…”
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Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor by Mbalaviele, Gabriel, Pauley, Adele M., Shaffer, Alexander F., Zweifel, Ben S., Mathialagan, Sumathy, Mnich, Stephen J., Nemirovskiy, Olga V., Carter, Jeff, Gierse, James K., Wang, Jane L., Vazquez, Michael L., Moore, William M., Masferrer, Jaime L.

“…Inflammation-induced microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal enzyme that synthesizes prostaglandin E 2 (PGE 2) downstream of…”
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Critical role for apoptosis signal-regulating kinase 1 in the development of inflammatory K/BxN serum-induced arthritis by Mnich, Stephen J., Blanner, Patrick M., Hu, Liangbiao G., Shaffer, Alexander F., Happa, Fernando A., O'Neil, Shawn, Ukairo, Okechukwu, Weiss, Dave, Welsh, Eric, Storer, Chad, Mbalaviele, Gabriel, Ichijo, Hidenori, Monahan, Joseph B., Hardy, Medora M., Eda, Hiroyuki

“…In this report, we show that apoptosis signal-regulating kinase 1 −/− (ASK1 KO) mice were resistant to inflammatory arthritis induced in the K/BxN serum…”
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4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, Valdecoxib:  A Potent and Selective Inhibitor of COX-2 by Talley, John J, Brown, David L, Carter, Jeffery S, Graneto, Matthew J, Koboldt, Carol M, Masferrer, Jaime L, Perkins, William E, Rogers, Roland S, Shaffer, Alexander F, Zhang, Yan Y, Zweifel, Ben S, Seibert, Karen

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Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: Use of a conformation-based hypothesis to facilitate compound design by Walker, Daniel P., Arhancet, Graciela B., Lu, Hwang-Fun, Heasley, Steven E., Metz, Sue, Kablaoui, Natasha M., Franco, Francisco M., Hanau, Cathleen E., Scholten, Jeffrey A., Springer, John R., Fobian, Yvette M., Carter, Jeffrey S., Xing, Li, Yang, Shengtian, Shaffer, Alexander F., Jerome, Gina M., Baratta, Michael T., Moore, William M., Vazquez, Michael L.

“…Microsomal prostaglandin E2 synthase-1 (mPGES-1) is a novel therapeutic target for the treatment of inflammation and pain. In the preceding letter, we detailed…”
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Comparative evaluation of arachidonic acid (AA)- and tetradecanoylphorbol acetate (TPA)-induced dermal inflammation by RAO, T. S, CURRIE, J. L, SHAFFER, A. F, ISAKSON, P. C

“…The effects of topical application of arachidonic acid (AA) or phorbol ester, tetradecanoylphorbol 13-acetate (TPA), on edema response, vascular permeability,…”
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Critical role for apoptosis signal-regulating kinase 1 in the development of inflammatory K/B×N serum-induced arthritis by MNICH, Stephen J, BLANNER, Patrick M, MBALAVIELE, Gabriel, ICHIJO, Hidenori, MONAHAN, Joseph B, HARDY, Medora M, EDA, Hiroyuki, HU, Liangbiao G, SHAFFER, Alexander F, HAPPA, Fernando A, O'NEIL, Shawn, UKAIRO, Okechukwu, WEISS, Dave, WELSH, Eric, STORER, Chad

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A novel, highly selective, tight binding IkappaB kinase-2 (IKK-2) inhibitor: a tool to correlate IKK-2 activity to the fate and functions of the components of the nuclear factor-kappaB pathway in arthritis-relevant cells and animal models by Mbalaviele, Gabriel, Sommers, Cynthia D, Bonar, Sheri L, Mathialagan, Sumathy, Schindler, John F, Guzova, Julia A, Shaffer, Alexander F, Melton, Michele A, Christine, Lori J, Tripp, Catherine S, Chiang, Po-Chang, Thompson, David C, Hu, Yiding, Kishore, Nandini

“…Nuclear factor (NF)-kappaB activation has been clearly linked to the pathogenesis of multiple inflammatory diseases including arthritis. The central role that…”
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Evaluation of 5-lipoxygenase inhibitors, zileuton, A-78773 and ICI-D-2138 in an ionophore (A-23187)-induced pleural inflammation model in the rat by Rao, T S, Currie, J L, Shaffer, A F, Isakson, P C

“…Intrapleural injection of A-23187 (10 micrograms), a calcium ionophore, elicited rapid increase in biosynthesis of prostaglandins and leukotrienes in a…”
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Role of mast cells in calcium ionophore (A23187)-induced peritoneal inflammation in mice by Rao, T S, Shaffer, A F, Currie, J L, Isakson, P C

“…Several lines of evidence document a critical role for mast cells in immune complex-mediated inflammatory models. However, their role in nonimmune models of…”
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