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Non-ATP Competitive Protein Kinase Inhibitors
Current Medicinal Chemistry, 2010 Protein kinases represent an attractive target in oncology drug discovery. Most of kinase inhibitors are ATP-competitive and are called type I inhibitors. The ATP-binding pocket is highly conserved among members of the kinase family and it is difficult to find selective agents.GARUTI, LAURA, ROBERTI, MARINELLA, G. Bottegoni +2 moreopenaire +4 more sourcesNon-kinase targets of protein kinase inhibitors
Nature Reviews Drug Discovery, 2017 Kinome-wide profiling platforms have comprehensively identified the relevant kinases that are targeted by numerous protein kinase inhibitors. However, recent projects have begun to discover non-kinase targets of kinase inhibitors. These non-kinase targets can contribute to the desired or undesired activities of inhibitors, or act as silent bystanders ...openaire +2 more sourcesBacterial protein kinase inhibitors
Drug Development Research, 2010 AbstractProtein kinases have become the second most important group of drug targets for the pharmaceutical industry next to G‐protein‐coupled receptors. Thus, over the past decade, a significant number of small molecules have been generated for protein kinase drug optimization programs. The vast majority of kinase inhibitors target the ATP binding site Michio Kurosu, Eeshwaraiah Begariopenaire +1 more sourceRottlerin, a Novel Protein Kinase Inhibitor
Biochemical and Biophysical Research Communications, 1994 Rottlerin, a compound from Mallotus philippinensis, is shown to inhibit protein kinases with some specificity for PKC. To some extent, the novel inhibitor is able to differentiate between PKC isoenzymes, with IC50 values for PKC delta of 3-6 microM, PKC alpha,beta,gamma of 30-42 microM and PKC epsilon,eta,zeta of 80-100 microM.M, Gschwendt, H J, Müller, K, Kielbassa, R, Zang, W, Kittstein, G, Rincke, F, Marks +6 moreopenaire +2 more sourcesProtein Kinase Inhibitors
2010 R. Hamish McAllister-Williams, Daniel Bertrand, Hans Rollema, Raymond S. Hurst, Linda P. Spear, Tim C. Kirkham, Thomas Steckler, Delphine Capdevielle, Jean-Philippe Boulenger, Delphine Capdevielle, Jean-Philippe Boulenger, Delphine Capdevielle, Jean-Philippe Boulenger, Cyril Höschl, Martine Cador, Ben J. Harrison, Christos Pantelis, Anthony Riley, Steve Kohut, Alex Hofer, Ben J. Harrison, Christos Pantelis, Seithikurippu R. Pandi-Perumal, D. Warren Spence, Shelby Freedman Harris, Michael J. Thorpy, Milton Kramer, Ian Stolerman, Holden D. Brown, Michael Ragozzino, Klaus A. Miczek, Anne Jackson, Sven Ove Ögren, Oliver Stiedl, Paul R. Pentel, Mark LeSage, Victoria L. Harvey, Tony Dickenson, Christine A. Franco, Marc N. Potenza, Gail Winger, Mei-Chuan Ko, James H. Woods, Matthew I. Palmatier, Rick A. Bevins, Stephan G. Anagnostaras, Jennifer R. Sage, Stephanie A. Carmack, Jos Prickaerts, Jos Prickaerts, Jos Prickaerts, Warren H. Meck, Catalin V. Buhushi, Christoph U. Correll, Ian Stolerman, Mohammed Shoaib, Trevor Robbins, Daniel Hoyer, Thomas Steckler, Linda P. Spear, Luzio Tremolizzo, Gessica Sala, Carlo Ferrarese, Seiya Miyamoto, Thomas Steckler, David S. Tait, Verity J. Brown, Richard A. Depue, Tara L. White, Craig A. Erickson, David J. Posey, Kelly Blankenship, Kimberly A. Stigler, Christopher J. McDougle, Craig A. Erickson, David J. Posey, Kelly Blankenship, Kimberly A. Stigler, Christopher J. McDougle, Ian Stolerman, Jean-Michel Scherrmann, S. Stevens Negus, Dana E. Selley, Laura J. Sim-Selley, Christoph Hiemke, Sophie Tambour, John C. Crabbe, Pierre Baumann, Kim Wolff, Christof Baltes, Thomas Mueggler, Markus Rudin, Alan J. Budney, Robert L. Balster, Sharon Walsh, Robert L. Balster, Sharon Walsh, Robert L. Balster, Sharon Walsh, Andrea Bari, Johannes Mosbacher, Paul Willner, Klaus A. Miczek, Trevor Robbins, Wolfgang Fleischhacker, Etienne Sibille, Nicole Edgar, Sabine M. Hölter, John F. Cryan, Michel Le Moal, Marco Leyton, Sara Tomlinson, Glen Baker, Bernard Le Foll, Naheed (Max) Mirza, Tomasz Schneider, Jos Prickaerts, Jos Prickaerts, Robert L. Balster, Sharon Walsh, Yogita Chudasama, Thomas Steckler, Thomas Steckler, Daniel Hoyer, Stan Floresco, Christine A. Franco, Marc Potenza, Fabrizio Benedetti, Peter Riederer, Siegfried Hoyer, Luzio Tremolizzo, Gessica Sala, Carlo Ferrarese, Luzio Tremolizzo, Gessica Sala, Carlo Ferrarese, Lucio Tremolizzo, Gessica Sala, Carlo Ferrarese, Arthur Christopoulos, Gregory D. Stewart, Patrick M. Sexton, Christoph Hiemke, Malcolm Lader, Stefan Leucht, Mark Slifstein, Linda P. Spear, Samuel G. Siris, Susan Jones, Peter Verheart, Per Svenningsson, Per Andrén, Seithikurippu R. Pandi-Perumal, Milton Kramer, Michael J. Thorpy, Shelby Freedman Harris, D. Warren Spence, John Atack, Hilde Lavreysen, Stephen C. Fowler, Harriet de Wit, Britta Hahn, Stephen C. Fowler, Helen Cassaday, Paul Willner, Darren R. Christensen, Warren K. Bickel, Michael Minzenberg, David Baldwin, C. Neill Epperson, C. Neill Epperson, Lawrence Scahill, I. T. Uzbay, Lisiane Bizarro, Bart Ellenbroek, Linda P. Spear, Patrick D. McGorry, Alison R. Yung, Mark A. Geyer, Johannes Mosbacher, Malcolm Lader, Angela Roberts, Celia Morgan, Valerie Curran, Christine A. Franco, Marc Potenza, Celia Morgan, Valerie Curran, Thomas Steckler, Harriet de Wit, Jill B. Becker, Mary Cain, Michael T. Bardo, Thomas Steckler, Trevor Robbins, Theodora Duka, Sam Hutton, C. Neill Epperson, Celia Morgan, Valerie Curran +199 moreopenaire +2 more sources