Cell Signalling - Part 2

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  • Created by: Lydia
  • Created 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
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What is the function of the extracellular domain of a receptor tyrosine kinase?
Specific ligand binding
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What is the function of the intracellular domain of a receptor tyrosine kinase?
Relay and amplify signals
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How many families of receptor tyrosine kinases are there?
9
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What is ErbB?
Family of receptor tyrosine kinases that bind growth factors and consist of Her1 (EGFR) /Her2/3/4
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Name 3 ligands ErbB-1 / HER1 binds
EGF, transforming growth factor alpha, regulins
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What are the ligands for HER2?
None have been discovered
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What are the effects of ErbB-3 homodimers?
No signalling
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What are the effects of ErbB-1 homodimers?
Weak signalling
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What are the effects of ErbB-4 homodimers?
Weak signalling
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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
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Name 4 features of ErbB-2 heterodimers
Slow ligand dissociation, relaxed ligand specificity, rapid recycling and prolonged firing
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What is exposed when a ligand binds to ErbB-1?
The dimerisation site
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What are the 3 main sections of a tyrosine kinase domain?
N-lobe, C-lobe and activation loop
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On EGFRs what is the special activation called where the N-lobe binds to the C-lobe of another?
Allosteric activation
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On the RTK, why are tyrosine residues phosphorylated in a sequence specific manner?
So there is a docking site for a specific signalling molecule
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What does MET tyrosine kinase stimulate?
Cell scattering, invasion, protection from apoptosis and angiogenesis
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Name a ligand of the MET receptor
Hepatocyte growth factor
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What is the name of the domain which binds to phosphorylated tyrosine kinase?
SH-2 domain
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Herceptin is a therapeutic antibody which binds what?
ErbB-2
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What is the equivalent of herceptin for the ErbB-1 receptor?
Cetuximab
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What domain does oncogenic ErbB-1 lack?
Extracellular
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Which site do HER2/ EGFRs tyrosine kinase inhibitors block?
ATP binding site
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Name a HER2 tyrosine kinase inhibitor
Iressa (getfitinib) and tarceva (erlotinib)
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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
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Other cards in this set

Card 2

Front

What is the function of the extracellular domain of a receptor tyrosine kinase?

Back

Specific ligand binding

Card 3

Front

What is the function of the intracellular domain of a receptor tyrosine kinase?

Back

Preview of the front of card 3

Card 4

Front

How many families of receptor tyrosine kinases are there?

Back

Preview of the front of card 4

Card 5

Front

What is ErbB?

Back

Preview of the front of card 5
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