Search Results - "Favata, Margaret F"

Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050 by Fridman, Jordan S, Scherle, Peggy A, Collins, Robert, Burn, Timothy C, Li, Yanlong, Li, Jun, Covington, Maryanne B, Thomas, Beth, Collier, Paul, Favata, Margaret F, Wen, Xiaoming, Shi, Jack, McGee, Ryan, Haley, Patrick J, Shepard, Stacey, Rodgers, James D, Yeleswaram, Swamy, Hollis, Greg, Newton, Robert C, Metcalf, Brian, Friedman, Steven M, Vaddi, Kris

“…Inhibiting signal transduction induced by inflammatory cytokines offers a new approach for the treatment of autoimmune diseases such as rheumatoid arthritis…”
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Inhibition of MAP Kinase Kinase Prevents Cytokine and Prostaglandin E2 Production in Lipopolysaccharide-Stimulated Monocytes by Scherle, Peggy A, Jones, Elizabeth A, Favata, Margaret F, Daulerio, Andrea J, Covington, Maryanne B, Nurnberg, Sherrill A, Magolda, Ronald L, Trzaskos, James M

“…Activation of the extracellular signal-regulated kinase (ERK) pathway has been shown to occur in monocytes following stimulation with LPS. However, the…”
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Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors by Wityak, John, Hobbs, Frank W., Gardner, Daniel S., Santella, Joseph B., Petraitis, Joseph J., Sun, Jung-Hui, Favata, Margaret F., Daulerio, Andrea J., Horiuchi, Kurumi Y., Copeland, Robert A., Scherle, Peggy A., Jaffe, Bruce D., Trzaskos, James M., Magolda, Ronald L., Trainor, George L., Duncia, John V.

“…Employing phenylmalonitrile dianion chemistry, a large number of analogues of MEK inhibitor lead SH053 (IC 50=140 nM) were rapidly synthesized leading to…”
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Identification of a Novel Inhibitor of Mitogen-activated Protein Kinase Kinase by Favata, M F, Horiuchi, K Y, Manos, E J, Daulerio, A J, Stradley, D A, Feeser, W S, Van Dyk, D E, Pitts, W J, Earl, R A, Hobbs, F, Copeland, R A, Magolda, R L, Scherle, P A, Trzaskos, J M

“…The compound U0126 (1,4-diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene) was identified as an inhibitor of AP-1 transactivation in a cell-based…”
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A High-Throughput Fluorescent Polarization Assay for Nuclear Receptor Binding Utilizing Crude Receptor Extract by Lin, Siqi, Bock, Cindy L., Gardner, Debra B., Webster, Jeffery C., Favata, Margaret F., Trzaskos, James M., Oldenburg, Kevin R.

“…A homogenous high-throughput assay has been developed to measure the binding between nuclear receptors and test compounds. This assay applies a fluorescence…”
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Inhibition of Mitogen-Activated Protein Kinase Kinase Blocks T Cell Proliferation But Does Not Induce or Prevent Anergy by DeSilva, Dimuthu R, Jones, Elizabeth A, Favata, Margaret F, Jaffee, Bruce D, Magolda, Ronald L, Trzaskos, James M, Scherle, Peggy A

“…Three mitogen-activated protein kinase pathways are up-regulated during the activation of T lymphocytes, the extracellular signal-regulated kinase (ERK), Jun…”
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MEK inhibitors: The chemistry and biological activity of U0126, its analogs, and cyclization products by Duncia, John V., Santella, Joseph B., Higley, C.Anne, Pitts, William J., Wityak, John, Frietze, William E., Rankin, F.Wayne, Sun, Jung-Hui, Earl, Richard A., Tabaka, A.Christine, Teleha, Christopher A., Blom, Karl F., Favata, Margaret F., Manos, Elizabeth J., Daulerio, Andrea J., Stradley, Deborah A., Horiuchi, Kurumi, Copeland, Robert A., Scherle, Peggy A., Trzaskos, James M., Magolda, Ronald L., Trainor, George L., Wexler, Ruth R., Hobbs, Frank W., Olson, Richard E.

“…In search of antiinflammatory drugs with a new mechanism of action, U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive…”
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The Extracellular Signal-Regulated Kinase Cascade Is Required for NMDA Receptor-Independent LTP in Area CA1 But Not Area CA3 of the Hippocampus by Kanterewicz, Beatriz I, Urban, Nathan N, McMahon, David B. T, Norman, Eric D, Giffen, Laura J, Favata, Margaret F, Scherle, Peggy A, Barrionuevo, German, Klann, Eric

“…Activation of extracellular signal-regulated kinase (ERK) has been shown to be necessary for NMDA receptor-dependent long-term potentiation (LTP). We studied…”
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Receptor density dictates the behavior of a subset of steroid ligands in glucocorticoid receptor-mediated transrepression by Zhao, Qihong, Pang, Jian, Favata, Margaret F., Trzaskos, James M.

“…By co-expressing glucocorticoid receptor (GR) and transcriptional reporter systems in GR-deficient Cos-7 cells, we profiled potency and efficacy of a panel of…”
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Inhibition of MAP Kinase Kinase (MEK) Results in an Anti-inflammatory Response in Vivo by Jaffee, Bruce D., Manos, Elizabeth J., Collins, Robert J., Czerniak, Phillip M., Favata, Margaret F., Magolda, Ronald L., Scherle, Peggy A., Trzaskos, James M.

“…The MAP kinase pathway has been well-characterized as a cascade of sequential protein phosphorylation events leading to the upregulation of a variety of genes…”
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Lymphocyte activating factor promotes T-cell growth factor production by cloned marine lymphoma cells by Smith, Kendall A, Gilbride, Kevin J, Favata, Margaret F

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Substrate-based inhibitors of lanosterol 14.alpha.-methyl demethylase: I. Assessment of inhibitor structure-activity relationship and cholesterol biosynthesis inhibition properties by Trzaskos, James M, Ko, Soo S, Magolda, Ronald L, Favata, Margaret F, Fischer, Robert T, Stam, Simon H, Johnson, Paul R, Gaylor, James L

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Substrate-based inhibitors of lanosterol 14 alpha-methyl demethylase: I. Assessment of inhibitor structure-activity relationship and cholesterol biosynthesis inhibition properties by Trzaskos, J M, Ko, S S, Magolda, R L, Favata, M F, Fischer, R T, Stam, S H, Johnson, P R, Gaylor, J L

“…A series of 15-, 32-, and 15,32-substituted lanost-8-en-3 beta-ols is described which function as inhibitors of cholesterol biosynthesis. These agents inhibit…”
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Modulation of 3-hydroxy-3-methylglutaryl-CoA reductase by 15 alpha-fluorolanost-7-en-3 beta-ol. A mechanism-based inhibitor of cholesterol biosynthesis by Trzaskos, J.M., Magolda, R.L., Favata, M.F., Fischer, R.T., Johnson, P.R., Chen, H.W., Ko, S.S., Leonard, D.A., Gaylor, J.L.

“…The chemical synthesis and metabolic characteristics of the lanosterol analogue, 15 alpha-fluorolanost-7-en-3 beta-ol, are described. The 15 alpha-fluorosterol…”
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