Protein Tyrosine Kinases as Targets for Cancer and Other Indications

摘要: The identification and characterization of the members individual signal transduction cascades, advances in understanding how these signals are integrated normal pathological conditions have provided new strategies for therapeutic intervention. Rapid progress has occurred last few years development inhibitors that target protein tyrosine kinases (PTKs), enzymes transfer γ-phosphate group adenosine triphosphate (ATP) to hydroxyl residues on proteins. Although PTKs represent a small percentage total number “kinome,” 90 518, disproportional currently clinical trials directed against them; e.g., more than 20 different being evaluated as potential targets oncology. There reasons why been considered be good targets. Epistatically, located upstream downstream tumor suppressor genes or oncogenes demonstrated play central roles apoptosis, proliferation, invasion, differentiation (1). Aberrant activation kinases, owing mutation overexpression, is sufficient them become transforming cellular animal models. majority receptor (RPTKs), deregulating mutations over half known RPTKs associated with human malignancies; see Table 1 examples. Finally, equally important epidemiological biochemical data, prevalence because fact they druggable.