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GPCR (G-proteins ((interactions anchor protein), Hydrophobic interactions…
GPCR
G-proteins
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Hydrophobic interactions between membrane and N-terminal of alpha subunit and C-terminal of y-subunit
Effector proteins: likely enzyme, 1st messenger can activate multiple G-proteins can activate multiple effectors
Heterotrimeric, located close to IC receptor side
GPCR activation activates GRK -> arrestin binding -> GP uncoupling + receptor internalisatization in clathrin coated pits
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Structure
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EC N-terminus, IC C-terminus
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By-subunits
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Alpha coupling, receptor affinity, downstream effector systems, regulate receptor phosphorylation by kinases
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Receptor states
Inverse agonists exclusively bind (propanolol, timolol)
R=active form of receptor, r=inactive
Agonists exclusively bind R, increase (R+LIG.R)
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Receptor dimerisation
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Heterodimers - GABA(B) needs 2, may have hybrid effects
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Disulphine (weak bond->mirrors), coiled coil interactions, transmembrane interactions.
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