BIO 320 Lecture Notes - Lecture 10: Epidermal Growth Factor Receptor, Tyrosine, Conformational Change
Document Summary
Enzyme-coupled receptors - cytosolic side/domain is enzyme or binds an enzyme - (receptor. Kinases - receptor on cytosolic side is kinase) Many extracellular signal proteins act through rtk and r(s/t)k. 3 specific residues that can be phosphorylated by kinases. Tyrosine (tyr, y) - receptor tyrosine kinase (rtk) - ~60 alleles. Regulate most aspects of cell survival and proliferation - central to human cancer (as well as differentiation and metabolism) Central to treatment and prevention of cancer. Ex: her2 egf receptor (epidermal growth factor receptor) - deregulated in various human cancers (become hyperactive - activate without ligand binding uncontrolled cell proliferation and cell survival) Activation - receptor dimerization (most common way to activate. Diffuse around membrane and encounter each other by chance - cannot phosphorylate each other (short encounter & inactive or very weakly active as monomer (acts slowly)) Almost all rtks - ligand binds and bridges monomers - brings kinase domains together (symmetrical) for longer time.
