Targeting protein kinases for tumor therapy.
Phosphorylation is the most common biochemical modification of cellular molecules, regulating fundamental cellular processes like growth, differentiation, proliferation, movement, and death. It is now clear that protein and lipid kinases as well as phosphatases are causally involved in human disease, especially in cancer. The first part of this review tries to compile our current knowledge about the involvement of protein kinases in human cancer. Phosphatases as well as phospholipid kinases will be omitted from this article for the purpose of simplification. In the second part an updated list of ongoing clinical trials involving protein kinases as targets for tumor therapy will be given, together with a brief summary of technical approaches in targeting protein kinases for therapy.
Sachsenmaier
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KTB Tumorforschungsgesellschaft mbH, Klinik für Tumorbiologie, Freiburg, Germany. sachsenm@tumorbio.uni-freiburg.de
D000970:Antineoplastic Agents / Q000009:adverse effects / Q000627:therapeutic use*; D001549:Benzamides; D002455:Cell Division / Q000187:drug effects / Q000502:physiology; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D002986:Clinical Trials as Topic; D004791:Enzyme Inhibitors / Q000009:adverse effects / Q000627:therapeutic use*; D006801:Humans; D000068877:Imatinib Mesylate; D009369:Neoplasms / Q000188:drug therapy* / Q000503:physiopathology; D010879:Piperazines / Q000009:adverse effects / Q000627:therapeutic use; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000502:physiology; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000502:physiology; D011743:Pyrimidines / Q000009:adverse effects / Q000627:therapeutic use; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000502:physiology
D000970:Antineoplastic Agents; D001549:Benzamides; D004791:Enzyme Inhibitors; D010879:Piperazines; D011743:Pyrimidines; D000068877:Imatinib Mesylate; D011505:Protein-Tyrosine Kinases; D020794:Receptor Protein-Tyrosine Kinases; D017346:Protein Serine-Threonine Kinases