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Receptor Tyrosine Kinase Inhibitors

Receptor tyrosine kinase inhibitors (RTKIs) are bioactive, usually aromatic, small molecules that are desirable drug targets as therapy for cancer, inflammatory, metabolic, proliferative and neurodegenerative diseases. Receptor tyrosine kinase inhibitors can bind to the active site of a RTK thus preventing phosphorylation and by doing so inhibit, regulate or modulate signaling, often with cytostatic activity. Some potent kinase inhibitors will exhibit selectivity for a certain RTK, while others are less selective. For example, some tyrphostins are potent and selective inhibitors of Vascular Endothelial Growth Factor Receptor (VEGFR) receptor kinases, but weak inhibitors of Platelet Derived Growth Factor Receptor (PDGFR) tyrosine kinases and Epidermal Growth Factor Receptor (EGFR) tyrosine kinases.