Non-Receptor Tyrosine Kinase Inhibitors

Non-receptor tyrosine kinase inhibitors (NRTKIs) are bioactive, usually aromatic, small molecules that are desirable drug targets as therapy for cancer, inflammatory, metabolic, proliferative and neurodegenerative diseases. Nonreceptor tyrosine kinase inhibitors bind to the active site of a non-receptor tyrosine kinase, 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 protein tyrosine kinases, while others are less selective. For example, LFM-A13 inhibits non-receptor Bruton′s tyrosine kinase (Btk), targeting lymphomas and autoimmune disorders, but also inhibits JAK1, JAK2, EGFR, IRK, IKK, and CDK1, CDK2, and CDK3. Piceatannol inhibits Syk and Lck.