Search Results - "Adams, Jerry L."

GSK1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models by Hardwicke, Mary Ann, Oleykowski, Catherine A, Plant, Ramona, Wang, Jamin, Liao, Qiaoyin, Moss, Katherine, Newlander, Ken, Adams, Jerry L, Dhanak, Dashyant, Yang, Jingsong, Lai, Zhihong, Sutton, David, Patrick, Denis

“…The protein kinases, Aurora A, B, and C have critical roles in the regulation of mitosis and are frequently overexpressed or amplified in human tumors…”
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Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885 by KING, Alastair J, PATRICK, Denis R, HUGGER, Erin, LIFU WANG, KARRETH, Florian, LOUGHEED, Julie C, LEE, Jae, CHAU, David, STOUT, Thomas J, MAY, Earl W, ROMINGER, Cynthia M, SCHABER, Michael D, BATORSKY, Roberta S, LUSONG LUO, LAKDAWALA, Ami S, ADAMS, Jerry L, CONTRACTOR, Rooja G, SMALLEY, Keiran S. M, HERLYN, Meenhard, MORRISSEY, Michael M, TUVESON, David A, HUANG, Pearl S, HO, Maureen L, DO, Hieu T, SHU YUN ZHANG, KUMAR, Rakesh, RUSNAK, David W, TAKLE, Andrew K, WILSON, David M

“…Oncogenic BRAF alleles are both necessary and sufficient for cellular transformation, suggesting that chemical inhibition of the activated mutant protein…”
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SB 239063, a p38 MAPK inhibitor, reduces neutrophilia, inflammatory cytokines, MMP-9, and fibrosis in lung by Underwood, D C, Osborn, R R, Bochnowicz, S, Webb, E F, Rieman, D J, Lee, J C, Romanic, A M, Adams, J L, Hay, D W, Griswold, D E

“…The effects of a second generation p38 mitogen-activated protein kinase (MAPK) inhibitor, SB 239063…”
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Structural basis of inhibitor selectivity in MAP kinases by Wang, Zhulun, Canagarajah, Bertram J, Boehm, Jeffrey C, Kassisà, Skouki, Cobb, Melanie H, Young, Peter R, Abdel-Meguid, Sherin, Adams, Jerry L, Goldsmith, Elizabeth J

“…Background: The mitogen-activated protein (MAP) kinases are important signaling molecules that participate in diverse cellular events and are potential targets…”
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Big opportunities for small molecules in immuno-oncology by Adams, Jerry L., Smothers, James, Srinivasan, Roopa, Hoos, Axel

“…Key Points The concept of immuno-oncology, using the immune system to fight cancer, dates back 150 years. However, broad clinical success for immunotherapies…”
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Optimization of triarylimidazoles for Tie2: Influence of conformation on potency by Johnson, Neil W., Semones, Marcus, Adams, Jerry L., Hansbury, Michael, Winkler, Jim

“…Optimization of triarylimidazoles for Tie2 potency resulted in the identification of the potent and selective tetrasubstituted imidazole 23 that was…”
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Potent and Selective Nonpeptide Inhibitors of Caspases 3 and 7 by Lee, Dennis, Long, Scott A, Murray, Jeffrey H, Adams, Jerry L, Nuttall, Mark E, Nadeau, Daniel P, Kikly, Kristine, Winkler, James D, Sung, Chiu-Mei, Ryan, M. Dominic, Levy, Mark A, Keller, Paul M, DeWolf, Walter E

“…5-Dialkylaminosulfonylisatins have been identified as potent, nonpeptide inhibitors of caspases 3 and 7. The most active compound within this series (34)…”
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Role of p38 Mitogen-Activated Protein Kinase in Rhinovirus-Induced Cytokine Production by Bronchial Epithelial Cells by Griego, Sandra D, Weston, Cynthia B, Adams, Jerry L, Tal-Singer, Ruth, Dillon, Susan B

“…The stress-activated protein kinase p38 plays a central role in the regulation of cytokine biosynthesis by various cell types in response to a wide range of…”
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Hypertensive end-organ damage and premature mortality are p38 mitogen-activated protein kinase-dependent in a rat model of cardiac hypertrophy and dysfunction by BEHR, Thomas M, NERURKAR, Sandhya S, OHLSTEIN, Eliot H, ANGERMANN, Christiane E, ADAMS, Jerry L, SISKO, Joseph, SACKNER-BERNSTEIN, Jonathan D, WILLETTE, Robert N, NELSON, Allen H, COATNEY, Robert W, WOODS, Tina N, SULPIZIO, Anthony, CHANDRA, Sudeep, BROOKS, David P, KUMAR, Sanjay, LEE, John C

“…Numerous pathological mediators of cardiac hypertrophy (eg, neurohormones, cytokines, and stretch) have been shown to activate p38 MAPK. The purpose of the…”
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Inhibition of p38 MAP kinase as a therapeutic strategy by Lee, John C, Kumar, Sanjay, Griswold, Don E, Underwood, David C, Votta, Bartholomew J, Adams, Jerry L

“…Since the discovery of p38 MAP kinase in 1994, our understanding of its biology has progressed dramatically. The key advances include (1) identification of p38…”
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Discovery of GSK1070916, a Potent and Selective Inhibitor of Aurora B/C Kinase by Adams, Nicholas D, Adams, Jerry L, Burgess, Joelle L, Chaudhari, Amita M, Copeland, Robert A, Donatelli, Carla A, Drewry, David H, Fisher, Kelly E, Hamajima, Toshihiro, Hardwicke, Mary Ann, Huffman, William F, Koretke-Brown, Kristin K, Lai, Zhihong V, McDonald, Octerloney B, Nakamura, Hiroko, Newlander, Ken A, Oleykowski, Catherine A, Parrish, Cynthia A, Patrick, Denis R, Plant, Ramona, Sarpong, Martha A, Sasaki, Kosuke, Schmidt, Stanley J, Silva, Domingos J, Sutton, David, Tang, Jun, Thompson, Christine S, Tummino, Peter J, Wang, Jamin C, Xiang, Hong, Yang, Jingsong, Dhanak, Dashyant

“…The Aurora kinases play critical roles in the regulation of mitosis and are frequently overexpressed or amplified in human tumors. Selective inhibitors may…”
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Metabolism and disposition of oral dabrafenib in cancer patients: proposed participation of aryl nitrogen in carbon-carbon bond cleavage via decarboxylation following enzymatic oxidation by Bershas, David A, Ouellet, Daniele, Mamaril-Fishman, Donna B, Nebot, Noelia, Carson, Stanley W, Blackman, Samuel C, Morrison, Royce A, Adams, Jerry L, Jurusik, Kristen E, Knecht, Dana M, Gorycki, Peter D, Richards-Peterson, Lauren E

“…A phase I study was conducted to assess the metabolism and excretion of [(14)C]dabrafenib (GSK2118436;…”
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Pyridinylimidazole inhibitors of Tie2 kinase by Semones, Marcus, Feng, Yanhong, Johnson, Neil, Adams, Jerry L., Winkler, Jim, Hansbury, Michael

“…The synthesis and in-depth evaluation of compound 5, an inhibitor (IC 50 = 250 nM) of Tie2 kinase, is described. This communication details the evolution of…”
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p38 Mitogen-Activated Protein Kinase Inhibitors— Mechanisms and Therapeutic Potentials by Lee, John C., Kassis, Shouki, Kumar, Sanjay, Badger, Alison, Adams, Jerry L.

“…The pyridinylimidazole compounds, exemplified by SB 203580, originally were prepared as inflammatory cytokine synthesis inhibitors. Subsequently, the compounds…”
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SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence by Underwood, D C, Osborn, R R, Kotzer, C J, Adams, J L, Lee, J C, Webb, E F, Carpenter, D C, Bochnowicz, S, Thomas, H C, Hay, D W, Griswold, D E

“…The anti-inflammatory/antiallergic activity of a novel second-generation p38 mitogen-activated protein kinase inhibitor, SB…”
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Pyridinyl Imidazole Inhibitors of p38 Mitogen-activated Protein Kinase Bind in the ATP Site by Young, P R, McLaughlin, M M, Kumar, S, Kassis, S, Doyle, M L, McNulty, D, Gallagher, T F, Fisher, S, McDonnell, P C, Carr, S A, Huddleston, M J, Seibel, G, Porter, T G, Livi, G P, Adams, J L, Lee, J C

“…The site of action of a series of pyridinyl imidazole compounds that are selective inhibitors of p38 mitogen-activated protein kinase in vitro and block…”
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Identification of a Selective Nonpeptide Antagonist of the Anaphylatoxin C3a Receptor That Demonstrates Antiinflammatory Activity in Animal Models by Ames, Robert S, Lee, Dennis, Foley, James J, Jurewicz, Anthony J, Tornetta, Mark A, Bautsch, Wilfried, Settmacher, Britta, Klos, Andreas, Erhard, Karl F, Cousins, Russell D, Sulpizio, Anthony C, Hieble, J. Paul, McCafferty, Gerald, Ward, Keith W, Adams, Jerry L, Bondinell, William E, Underwood, David C, Osborn, Ruth R, Badger, Alison M, Sarau, Henry M

“…The anaphylatoxin C3a is a potent chemotactic peptide and inflammatory mediator released during complement activation which binds to and activates a…”
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Two convenient regioselective syntheses of 1- N-alkyl-3-aryl-4-[pyrimidin-4-yl]-pyrazoles by Ralph, Jeffrey M., Faitg, Thomas H., Silva, Domingos J., Feng, Yanhong, Blackledge, Charles W., Adams, Jerry L.

“…Two regioselective synthetic routes for 1- N-alkyl-3-aryl-4-[pyrimidin-4-yl]-pyrazoles of generic formula 1 were developed. These highly efficient and scalable…”
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Acquisition of Sensitivity of Stress-activated Protein Kinases to the p38 Inhibitor, SB 203580, by Alteration of One or More Amino Acids within the ATP Binding Pocket by Gum, R J, McLaughlin, M M, Kumar, S, Wang, Z, Bower, M J, Lee, J C, Adams, J L, Livi, G P, Goldsmith, E J, Young, P R

“…Pyridinyl imidazole inhibitors of p38 mitogen-activated protein kinase compete with ATP for binding. Mutation of 23 residues in the ATP pocket indicated that…”
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Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity by Adams, Jerry L., Boehm, Jeffrey C., Gallagher, Timothy F., Kassis, Shouki, Webb, Edward F., Hall, Ralph, Sorenson, Margaret, Garigipati, Ravi, Griswold, Don E., Lee, John C.

“…Optimization of a series of N-1-cycloalkyl-4-aryl-5-(pyrimidin-4-yl)imidazole inhibitors of p38 kinase is reported. Oral administration of inhibitors…”
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