Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases.

Journal article

Protein kinases are involved in many essential cellular processes and their deregulation can lead to a variety of diseases, including cancer. The pharmaceutical industry has invested heavily in the identification of kinase inhibitors to modulate these disease-promoting pathways, resulting in several successful drugs. However, the field is challenging as it is difficult to identify novel selective inhibitors with good pharmacokinetic/pharmacodynamic properties. In addition, resistance to kinas...

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Authors: Cowan-Jacob, S; Jahnke, W; Knapp, S

• Publication status: Published
• Publisher: Future Science
• Journal: Future medicinal chemistry
• Volume: 6
• Issue: 5
• Pages: 541-561
• Publication date: 2014-04-01
• DOI: 10.4155/fmc.13.216
• EISSN: 1756-8927
• ISSN: 1756-8919
• Language: English
• Keywords: Binding Sites; Surface Plasmon Resonance; Allosteric Site; Allosteric Regulation; Molecular Docking Simulation; Humans; Protein Kinase Inhibitors; Databases, Protein; Protein Kinases; Protein Structure, Tertiary; Pharmacokinetics