[Recent advances in development of antitumor tyrosine kinase inhibitors].
Protein tyrosine kinases are critical enzymes in regulating cellular growth and differentiation and are also deeply involved in oncogenesis since they are frequently activated in a variety of human cancers. Novel compounds that inhibit epidermal growth factor receptors (EGF-R) with high specificity and potency were developed, and their antitumor effects on EGF-R overexpressing cells and in vivo tumor models were demonstrated. Novel compounds that preferentially inhibit human glioma cells expressing truncated rather than wild-type EGF-R were also developed. Tyrphostin analogs which inhibit angiogenesis and thereby suppress tumor cell growth were also identified by screening inhibitors of Flk-1 tyrosine kinase.
Uehara
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National Institute of Infectious Diseases.
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000494:pharmacology; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D009369:Neoplasms / Q000473:pathology; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D017978:Receptors, Growth Factor / Q000037:antagonists & inhibitors; D040262:Receptors, Vascular Endothelial Growth Factor
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D017978:Receptors, Growth Factor; D066246:ErbB Receptors; D011505:Protein-Tyrosine Kinases; D020794:Receptor Protein-Tyrosine Kinases; D040262:Receptors, Vascular Endothelial Growth Factor