OnCo
termsTerm

Kinase

aka kinases, tyrosine kinase, tyrosine kinases, protein kinase, protein kinases, kinase domain, tyrosine kinase inhibitor, tyrosine kinase inhibitors, TKI, TKIs

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; many 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.

Category
Biology basics

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