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16 Cards in this Set
- Front
- Back
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GPCR |
G-protein coupled receptor. |
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G-protein |
act as a molecular switch |
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Heterotrimeric |
binds guanine nucleotides. GTPase enzyme. stable complex associated with membrane. |
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Gs(alpha(s)beta,gamma) |
stimulates adenylyl cyclase |
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Gi(alpha(i)beta,gamma) |
inhibits adenylyl cyclase |
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Gq(alpha(q)beta,gamma) |
activates phospholipase C |
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Adenylyl cyclase |
produces cyclic AMP |
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Phospholipase C |
produces IP3 and DAG . |
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cGMP |
produced by guanylyl cyclase & target Protein kinase G |
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cAMP |
targets Protein kinase A |
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DAG |
targets Protein kinase C |
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IP3 |
targets IP3 receptors = activation releases intracellular stores of Ca+. |
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Protein phosphorylation/dephosphorylation |
1. kinase enzyme recognise target sequence and add phosphate. 2. phosphatase enzyme removes phosphate. 3. act as switch to regulate physiological response. |
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cAMP transcription |
1. CREB bound to CRE 2. Activated PKA phosphorylates CREB. 3. CBP is recruited to transcription complex and initiates transcription. |
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GPCR Signalling cycle |
1. unstimulated state 2. receptor activation by agonist 3. receptor activation of G-protein 4. G-protein effector interaction and production of 2nd messenger 5. GTPase |
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Signal termination |
removal of second messenger. inactivation & deseitisin mechanisms |
