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27 Cards in this Set
- Front
- Back
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What does desensitisation involve |
Involved phosphorylation of the activated receptor by a specific kinase Phosphorylated receptor then binds to arrestin making it lose its ability to associate with G protein and undergo endocytosis- removing the receptor from the membrane |
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What is endocytosis |
the taking in of matter by a living cell by invagination of its membrane to form a vacuole |
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What is heterologous desensitisation |
Is a result if phosphorylation of one type of receptor as a result of activation of kinases by another PKA and PKC |
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What do GRKS phosphorylate |
Specific residues on the C terminal tail of GPCR |
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What does arrestin outcompete G protein for |
For site at receptor so lose G protein coupled signalling |
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What does arrestin promote |
Internalisation |
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What is salmeterol |
Long acting B2 agonist in asthma |
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What does salmeterol cause |
Less internalisation of the beta 2 adrenoceptor |
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What is a kinase linked receptor |
They mediate the actions of a wide variety of protein mediators including growth factors and cytokines and hormones such as insulin and leptin Effects are exerted mainly in the level of gene transcription |
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What does arrestin compete with for a sore at the receptor |
G protein so we loose GPC signalling |
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What does polymorphism give rise tk |
Multiple proteins, GPCR, receptor trafficking, changes in internalisation |
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How is IP3 inactivated |
By dephosphorylation by inositol phosphate phosphatases |
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What is vaptan |
V2 receptor Inverse agonist Binds to misfolded V2 mutant and helps it get to the plasma membrane Treatment for nephrogenic diabetes |
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What is the V2 mutation |
Doesn’t let basically press in fold properly- doesn’t make it out the ribosome |
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What does PDE type IV do inside cells of the airways |
Inhibition increase cAMP causing relaxation and dampens inflammation |
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What happens when we stop PDE4 inside the smooth muscle cells of the penis |
Increased cGMP causing relaxation and increased blood flow for erectile dysfunction aka viagra |
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What is the growth factor receptor pathway |
Growth factor bonds to growth factor revelry causing a intermolecular tyrosyl phosphorylation of the receptor This causes the recruitment of protein Grb-2 from the cytoplasm this then goes on to bind to msos via SH-3 domain Msos causes activation of proto oncogene termed p21ras by promoting the GDP-GTP exchange this protein Activated GTP bound p21ras in turn localised raf-1-kinase to the cell membrane This causes kinase cascade that activates mitogen activated kinase MAPK and catalysed phosphorylation and activation of p90rsk Activates MAPK and p90rsk translocates to the nucleus where it activates transcription factors This induces immediate early genes which provoke DNA synthesis and commit the cells to divide |
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What is PDE4 involved in |
Activation of inflammatory cells Its inhibitors are viable anti inflammatory drugs |
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How is IP3 inactivated |
By dephosphorylation by inositol phosphate phosphates |
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What can inflammatory diseases cause other than inflammation |
Increase cAMP phosphodiesterase activity which lowers cAMP |
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What is viagra |
CGMP phosphodiesterase inhibitor that is used to treat impotence |
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What is vaptan |
V2 receptor Inverse agonist Binds to misfolded V2 mutant and helps it get to the plasma membrane Treatment for nephrogenic diabetes |
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What is the V2 mutation |
Doesn’t let baso pressin fold properly- doesn’t make it out the ribosome |
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What is a loss of function mutation |
Block signalling in response to the corresponding agonist |
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What is a gain of function mutation |
Lead constitutive agonist independent activation of signalling |
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What is polymorphism |
More common single nucleotide change |
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What can PDE4 inhibitors be used to treat |
COPD and asthma |
