Kinase inhibitors in cancer therapy: a look ahead.
The most essential kinases involved in cell membrane receptor activation, signal transduction and cell cycle control or programmed cell death and their interconnections are reviewed. In tumours, the genes of many of those kinases are mutated or amplified or the proteins are overexpressed. The use of key kinases offers the possibility to screen in vitro for synthetic small molecule kinase inhibitors. In view of the many interconnections of cellular kinases, their role in preventing or inducing programmed cell death and the possibility that a considerable number of signal transducing proteins are still unknown, cellular test systems are recommended in which the respective key kinase or one of its main partner molecules are overexpressed.
Sedlacek
H H
HH
Aventis Pharma Deutschland GmbH, Central Biotechnology, Marburg, Germany. Hans-Harald.Sedlacek@aventis.com
D002453:Cell Cycle / Q000187:drug effects; D002462:Cell Membrane / Q000187:drug effects*; D066246:ErbB Receptors / Q000187:drug effects*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000209:etiology; D010770:Phosphotransferases / Q000009:adverse effects / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases / Q000009:adverse effects / Q000378:metabolism; D017346:Protein Serine-Threonine Kinases / Q000009:adverse effects / Q000037:antagonists & inhibitors / Q000378:metabolism; D011505:Protein-Tyrosine Kinases / Q000009:adverse effects / Q000037:antagonists & inhibitors / Q000378:metabolism; D017526:Receptor, IGF Type 1 / Q000187:drug effects; D015398:Signal Transduction / Q000187:drug effects*; D014158:Transcription, Genetic; D019061:src-Family Kinases / Q000009:adverse effects / Q000378:metabolism
D047428:Protein Kinase Inhibitors; D010770:Phosphotransferases; D011494:Protein Kinases; D066246:ErbB Receptors; D011505:Protein-Tyrosine Kinases; D017526:Receptor, IGF Type 1; D019061:src-Family Kinases; D017346:Protein Serine-Threonine Kinases