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An enzyme that switches other proteins on by sticking a phosphate group onto them. Cancer signalling runs on kinases, and kinase inhibitors are the biggest class of targeted drugs.
The human genome encodes about 500 kinases; a large share sit in growth pathways, including the inner part of receptors like EGFR and HER2 and the relay proteins BRAF, MEK, ALK, CDK4/6 and PI3K. A mutated kinase that stays permanently active is one of the commonest cancer drivers, and because kinases share a pocket that binds ATP (the phosphate donor), small molecules designed to occupy that pocket can shut them off. Imatinib against BCR-ABL in 2001 proved the idea; dozens of kinase inhibitors now exist, and successive generations are engineered to overcome the resistance mutations that arise in the pocket.
In plain words · A growth receptor that is mutated in some lung cancers and overproduced in others; the first great success of targeted pills.
Showing the target this term concerns: EGFR.
Shares Growth signal, Oncogene, Oncogene addiction, ALK.
Shares Growth signal, Receptor, Signalling pathway, EGFR.
Shares Lorlatinib, ALK, Osimertinib, EGFR.
Shares Lorlatinib, ALK, Osimertinib, EGFR.
Shares Lorlatinib, ALK, Osimertinib, EGFR.
Shares Cell cycle, CDK4/6, CDK4/6 inhibitors.
Shares Oncogene addiction, ALK, Imatinib, Osimertinib.
Shares Signalling pathway, Targeted therapy.