Cell Signalling - Part 2 0.0 / 5 ? BiologyCell Signalling and TherapeuticsUniversityNone Created by: LydiaCreated on: 06-12-17 19:19 What is a critical node? Points in a pathway that are critical for biological response. They have different isoforms allowing for divergence/ tissue specificity 1 of 25 What is the function of the extracellular domain of a receptor tyrosine kinase? Specific ligand binding 2 of 25 What is the function of the intracellular domain of a receptor tyrosine kinase? Relay and amplify signals 3 of 25 How many families of receptor tyrosine kinases are there? 9 4 of 25 What is ErbB? Family of receptor tyrosine kinases that bind growth factors and consist of Her1 (EGFR) /Her2/3/4 5 of 25 Name 3 ligands ErbB-1 / HER1 binds EGF, transforming growth factor alpha, regulins 6 of 25 What are the ligands for HER2? None have been discovered 7 of 25 What are the effects of ErbB-3 homodimers? No signalling 8 of 25 What are the effects of ErbB-1 homodimers? Weak signalling 9 of 25 What are the effects of ErbB-4 homodimers? Weak signalling 10 of 25 What are the effects of heterodimers between ErbB-2 and ErbB1/3/4? Potent signalling leading to increased cell proliferation/ migration and resistance to apoptosis 11 of 25 Name 4 features of ErbB-2 heterodimers Slow ligand dissociation, relaxed ligand specificity, rapid recycling and prolonged firing 12 of 25 What is exposed when a ligand binds to ErbB-1? The dimerisation site 13 of 25 What are the 3 main sections of a tyrosine kinase domain? N-lobe, C-lobe and activation loop 14 of 25 On EGFRs what is the special activation called where the N-lobe binds to the C-lobe of another? Allosteric activation 15 of 25 On the RTK, why are tyrosine residues phosphorylated in a sequence specific manner? So there is a docking site for a specific signalling molecule 16 of 25 What does MET tyrosine kinase stimulate? Cell scattering, invasion, protection from apoptosis and angiogenesis 17 of 25 Name a ligand of the MET receptor Hepatocyte growth factor 18 of 25 What is the name of the domain which binds to phosphorylated tyrosine kinase? SH-2 domain 19 of 25 Herceptin is a therapeutic antibody which binds what? ErbB-2 20 of 25 What is the equivalent of herceptin for the ErbB-1 receptor? Cetuximab 21 of 25 What domain does oncogenic ErbB-1 lack? Extracellular 22 of 25 Which site do HER2/ EGFRs tyrosine kinase inhibitors block? ATP binding site 23 of 25 Name a HER2 tyrosine kinase inhibitor Iressa (getfitinib) and tarceva (erlotinib) 24 of 25 Name the regions of the ATP binding site that are important for drug specificity for drugs which target TKRs Adenine region, sugar region, hydrophobic pocket, hydrophobic channel and phosphate binding region 25 of 25
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