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What is the structure of ion channels?
4-5 subunits each with 4 membrane spanning alpha helices
Gated and open to form a pore
What are the type of ion channels?
Voltage gated
Ligand gated (extra/intra)
Mechanically gated
What is the structure of a GPCR?
single polypeptide with 7 transmembrane domains
Ligand binding domain and G-protein binding domain
How are GPCRs activated?
Ligand binds causing conformational change of receptor
activates the G-protein
alpha, beta and gamma subunits
alpha inactive with GDP
When activated alpha dissociates and activates downstream signalling
What is the function of G alpha S?
stimulates adenylyl cyclase which produces cAMP
What is the function of G alpha I?
Inhibits adenylyl cyclase so no cAMP produced
What is the function of G alpha q/11?
activates phospholipase C produce inositol triphosphate (IP3)hatW
What is the function of G beta and gamma?
Activate/inhibit ion channels
Activate kinases
What is the process followed by activation of G alpha S?
Activates adenylyl cyclase which produces cAMP from ATP
one target is protein kinase A (PKA)
this binding allows subunits of PKA to phosphorylate CREB
controls gene transcription
What is the process followed by activation of G alpha q/11?
Phospholipase C activation
produces IP3 and diacylglycerol which releases calcium in ER
diacylglycerol and calcium activate protein kinase C