The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901
Barrett, Stephen D., Bridges, Alexander J., Dudley, David T., Saltiel, Alan R., Fergus, James H., Flamme, Cathlin M., Delaney, Amy M., Kaufman, Michael, LePage, Sophie, Leopold, Wilbur R., Przybranowski, Sally A., Sebolt-Leopold, Judith, Van Becelaere, Keri, Doherty, Annette M., Kennedy, Robert M., Marston, Dan, Howard, W. Allen, Smith, Yvonne, Warmus, Joseph S., Tecle, Haile
Published in Bioorganic & medicinal chemistry (15.12.2008)
Published in Bioorganic & medicinal chemistry (15.12.2008)
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Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition
Hasemann, Charles A, Ohren, Jeffrey F, Chen, Huifen, Pavlovsky, Alexander, Whitehead, Christopher, Zhang, Erli, Kuffa, Peter, Yan, Chunhong, McConnell, Patrick, Spessard, Cindy, Banotai, Craig, Mueller, W Thomas, Delaney, Amy, Omer, Charles, Sebolt-Leopold, Judith, Dudley, David T, Leung, Iris K, Flamme, Cathlin, Warmus, Joseph, Kaufman, Michael, Barrett, Stephen, Tecle, Haile
Published in Nature structural & molecular biology (01.12.2004)
Published in Nature structural & molecular biology (01.12.2004)
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Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor
Gonzales, Andrea J, Hook, Kenneth E, Althaus, Irene W, Ellis, Paul A, Trachet, Erin, Delaney, Amy M, Harvey, Patricia J, Ellis, Teresa A, Amato, Danielle M, Nelson, James M, Fry, David W, Zhu, Tong, Loi, Cho-Ming, Fakhoury, Stephen A, Schlosser, Kevin M, Sexton, Karen E, Winters, R Thomas, Reed, Jessica E, Bridges, Alex J, Lettiere, Daniel J, Baker, Deborah A, Yang, Jianxin, Lee, Helen T, Tecle, Haile, Vincent, Patrick W
Published in Molecular cancer therapeutics (01.07.2008)
Published in Molecular cancer therapeutics (01.07.2008)
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Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo
Sebolt-Leopold, Judith S, Dudley, David T, Herrera, Roman, Becelaere, Keri Van, Wiland, Amy, Gowan, Richard C, Tecle, Haile, Barrett, Stephen D, Bridges, Alexander, Przybranowski, Sally, Leopold, W.R, Saltiel, Alan R
Published in Nature medicine (01.07.1999)
Published in Nature medicine (01.07.1999)
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Milameline (CI-979/RU35926): A Muscarinic Receptor Agonist with Cognition-Activating Properties: Biochemical and In Vivo Characterization
Schwarz, R D, Callahan, M J, Coughenour, L L, Dickerson, M R, Kinsora, J J, Lipinski, W J, Raby, C A, Spencer, C J, Tecle, H
Published in The Journal of pharmacology and experimental therapeutics (01.11.1999)
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Published in The Journal of pharmacology and experimental therapeutics (01.11.1999)
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Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4‑d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family
Smaill, Jeff B, Gonzales, Andrea J, Spicer, Julie A, Lee, Helen, Reed, Jessica E, Sexton, Karen, Althaus, Irene W, Zhu, Tong, Black, Shannon L, Blaser, Adrian, Denny, William A, Ellis, Paul A, Fakhoury, Stephen, Harvey, Patricia J, Hook, Ken, McCarthy, Florence O. J, Palmer, Brian D, Rivault, Freddy, Schlosser, Kevin, Ellis, Teresa, Thompson, Andrew M, Trachet, Erin, Winters, R. Thomas, Tecle, Haile, Bridges, Alexander
Published in Journal of medicinal chemistry (08.09.2016)
Published in Journal of medicinal chemistry (08.09.2016)
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Central role of the MEK/ERK MAP kinase pathway in a mouse model of rheumatoid arthritis: Potential proinflammatory mechanisms
Thiel, Melissa J., Schaefer, Caralee J., Lesch, Mark E., Mobley, James L., Dudley, David T., Tecle, Haile, Barrett, Stephen D., Schrier, Denis J., Flory, Craig M.
Published in Arthritis and rheumatism (01.10.2007)
Published in Arthritis and rheumatism (01.10.2007)
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2-Alkylamino-and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase)
WARMUS, Joseph S, FLAMME, Cathlin, MERRIMAN, Ronald, OHREN, Jeffrey, PAVLOVSKY, Alexander, PRZYBRANOWSKI, Sally, TECLE, Haile, VALIK, Heather, WHITEHEAD, Christopher, ERLI ZHANG, LU YAN ZHANG, BARRETT, Stephen, BRIDGES, Alexander, HUIFEN CHEN, GOWAN, Richard, KAUFMAN, Michael, SEBOLT-LEOPOLD, Judy, LEOPOLD, Wilbur
Published in Bioorganic & medicinal chemistry (01.12.2008)
Published in Bioorganic & medicinal chemistry (01.12.2008)
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Mutations of aspartate 103 in the Hm2 receptor and alterations in receptor binding properties of muscarinic agonists
Schwarz, Roy D., Spencer, Carolyn J., Jaen, Juan C., Mirzadegan, Tara, Moreland, David, Tecle, Haile, Thomas, Anthony J.
Published in Life sciences (1973) (1995)
Published in Life sciences (1973) (1995)
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Beyond the MEK-pocket: Can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?
Tecle, Haile, Shao, Jianxing, Li, Yanhong, Kothe, Michael, Kazmirski, Steven, Penzotti, Julie, Ding, Yuan-Hua, Ohren, Jeffrey, Moshinsky, Deb, Coli, Rocco, Jhawar, Nidhi, Bora, Emilia, Jacques-O’Hagan, Suzanne, Wu, Joe
Published in Bioorganic & medicinal chemistry letters (01.01.2009)
Published in Bioorganic & medicinal chemistry letters (01.01.2009)
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4-Anilino-5-carboxamido-2-pyridone Derivatives as Noncompetitive Inhibitors of Mitogen-Activated Protein Kinase Kinase
Spicer, Julie A, Rewcastle, Gordon W, Kaufman, Michael D, Black, Shannon L, Plummer, Mark S, Denny, William A, Quin, John, Shahripour, Aurash B, Barrett, Stephen D, Whitehead, Christopher E, Milbank, Jared B. J, Ohren, Jeffrey F, Gowan, Richard C, Omer, Charles, Camp, Heidi S, Esmaeil, Nadia, Moore, Kelley, Sebolt-Leopold, Judith S, Pryzbranowski, Sally, Merriman, Ronald L, Ortwine, Daniel F, Warmus, Joseph S, Flamme, Cathlin M, Pavlovsky, Alexander G, Tecle, Haile
Published in Journal of medicinal chemistry (18.10.2007)
Published in Journal of medicinal chemistry (18.10.2007)
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Enhanced selectivity profile of pyrazole-urea based DFG-out p38α inhibitors
Liu, Hu, Kuhn, Cyrille, Feru, Frederic, Jacques, Suzanne L., Deshmukh, Gayatri D., Ye, Ping, Rennie, Glen R., Johnson, Theresa, Kazmirski, Steven, Low, Simon, Coli, Rocco, Ding, Yuan-hua, Cheng, Alan C., Tecle, Haile, English, Jessie M., Stanton, Robert, Wu, Joe C.
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
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Journal Article
Enhanced selectivity profile of pyrazole-urea based DFG-out p38a inhibitors
Liu, Hu, Kuhn, Cyrille, Feru, Frederic, Jacques, Suzanne L, Deshmukh, Gayatri D, Ye, Ping, Rennie, Glen R, Johnson, Theresa, Kazmirski, Steven, Low, Simon, Coli, Rocco, Ding, Yuan-Hua, Cheng, Alan C, Tecle, Haile, English, Jessie M, Stanton, Robert, Wu, Joe C
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
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Erratum to “2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles— O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase)” [Bioorg. Med. Chem. Lett. 18 (2008) 6171]
Warmus, Joseph S., Flamme, Cathlin, Zhang, Lu Yan, Barrett, Stephen, Bridges, Alexander, Chen, Huifen, Gowan, Richard, Kaufman, Michael, Sebolt-Leopold, Judy, Leopold, Wilbur, Merriman, Ronald, Ohren, Jeffrey, Pavlovsky, Alexander, Przybranowski, Sally, Tecle, Haile, Valik, Heather, Whitehead, Christopher, Zhang, Erli
Published in Bioorganic & medicinal chemistry letters (01.07.2009)
Published in Bioorganic & medicinal chemistry letters (01.07.2009)
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N-(6,7-Dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-alkylsulfonamides as peripherally restricted N-methyl-d-aspartate receptor antagonists for the treatment of pain
Deur, Christopher, Agrawal, Arun K., Baum, Heidi, Booth, John, Bove, Susan, Brieland, Joan, Bunker, Amy, Connolly, Cleo, Cornicelli, Joseph, Dumin, JoAnn, Finzel, Barry, Gan, Xinmin, Guppy, Sheila, Kamilar, Gregg, Kilgore, Kenneth, Lee, Pil, Loi, Cho-Ming, Lou, Zhen, Morris, Mark, Philippe, Laurence, Przybranowski, Sally, Riley, Frank, Samas, Brian, Sanchez, Brian, Tecle, Haile, Wang, Ziqiang, Welch, Kathryn, Wilson, Michael, Yates, Karen
Published in Bioorganic & medicinal chemistry letters (15.08.2007)
Published in Bioorganic & medicinal chemistry letters (15.08.2007)
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Design, Synthesis and Potential Utility of Fluorescence Probes that Target DFG-out Conformation of p38α for High Throughput Screening Binding Assay
Tecle, Haile, Feru, Frederic, Liu, Hu, Kuhn, Cyrille, Rennie, Glen, Morris, Mark, Shao, Jiangxing, Cheng, Alan C, Gikunju, Diana, Miret, Juan, Coli, Rocco, Xi, Simon (Hualin), Clugston, Susan L, Low, Simon, Kazmirski, Steven, Ding, Yuan-Hua, Cao, Qing, Johnson, Theresa L, Deshmukh, Gayatri D, DiNitto, Jonathan P, Wu, Joe C, English, Jessie M
Published in Chemical biology & drug design (01.12.2009)
Published in Chemical biology & drug design (01.12.2009)
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Journal Article
Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors
Liu, Hu, Kuhn, Cyrille, Feru, Frederic, Jacques, Suzanne L, Deshmukh, Gayatri D, Ye, Ping, Rennie, Glen R, Johnson, Theresa, Kazmirski, Steven, Low, Simon, Coli, Rocco, Ding, Yuan-hua, Cheng, Alan C, Tecle, Haile, English, Jessie M, Stanton, Robert, Wu, Joe C
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
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Erratum: Corrigendum: Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition
Ohren, Jeffrey F, Chen, Huifen, Pavlovsky, Alexander, Whitehead, Christopher, Zhang, Erli, Kuffa, Peter, Yan, Chunhong, McConnell, Patrick, Spessard, Cindy, Banotai, Craig, Mueller, W Thomas, Delaney, Amy, Omer, Charles, Sebolt-Leopold, Judith, Dudley, David T, Leung, Iris K, Flamme, Cathlin, Warmus, Joseph, Kaufman, Michael, Barrett, Stephen, Tecle, Haile, Hasemann, Charles A
Published in Nature structural & molecular biology (01.03.2005)
Published in Nature structural & molecular biology (01.03.2005)
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Journal Article
Corrigendum: Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition
Ohren, Jeffrey F, Chen, Huifen, Pavlovsky, Alexander, Whitehead, Christopher, Zhang, Erli, Kuffa, Peter, Yan, Chunhong, McConnell, Patrick, Spessard, Cindy, Banotai, Craig, Mueller, W Thomas, Delaney, Amy, Omer, Charles, Sebolt-Leopold, Judith, Dudley, David T, Leung, Iris K, Flamme, Cathlin, Warmus, Joseph, Kaufman, Michael, Barrett, Stephen, Tecle, Haile, Hasemann, Charles A
Published in Nature structural & molecular biology (01.03.2005)
Published in Nature structural & molecular biology (01.03.2005)
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4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties
Jaen, Juan C, Wise, Lawrence D, Caprathe, Bradley W, Tecle, Haile, Bergmeier, Stephen, Humblet, Christine C, Heffner, Thomas G, Meltzer, Leonard T, Pugsley, Thomas A
Published in Journal of medicinal chemistry (01.01.1990)
Published in Journal of medicinal chemistry (01.01.1990)
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