Kinase inhibitors in cancer therapy : A look ahead

• Published in: Drugs (New York, N.Y.) Vol. 59; no. 3; pp. 435 - 476
• Main Author: SEDLACEK, H. H
• Format: Journal Article
• Language: English
• Published: Auckland Adis International 01.03.2000
• Subjects: Antineoplastic agents; Biological and medical sciences; Cell Cycle - drug effects; Cell Membrane - drug effects; Cell physiology; Cell transformation and carcinogenesis. Action of oncogenes and antioncogenes; Fundamental and applied biological sciences. Psychology; General aspects; Humans; Medical sciences; Molecular and cellular biology; Neoplasms - drug therapy; Neoplasms - etiology; Pharmacology. Drug treatments; Phosphotransferases - adverse effects; Phosphotransferases - antagonists & inhibitors; Phosphotransferases - genetics; Phosphotransferases - metabolism; Protein Kinase Inhibitors; Protein Kinases - adverse effects; Protein Kinases - metabolism; Protein-Serine-Threonine Kinases - adverse effects; Protein-Serine-Threonine Kinases - antagonists & inhibitors; Protein-Serine-Threonine Kinases - metabolism; Protein-Tyrosine Kinases - adverse effects; Protein-Tyrosine Kinases - antagonists & inhibitors; Protein-Tyrosine Kinases - metabolism; Receptor, Epidermal Growth Factor - drug effects; Receptor, IGF Type 1 - drug effects; Signal Transduction - drug effects; src-Family Kinases - adverse effects; src-Family Kinases - metabolism; Transcription, Genetic; Antineoplastic agent; Human; Enzyme; Pathogenesis; Transferases; Enzyme inhibitor; Review; Malignant tumor; Carcinogenesis; In vitro; In vivo; Protein kinase; Animal
• DOI: 10.2165/00003495-200059030-00004
• ISSN: 0012-6667

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.