Biological Signalling: GPCR Flashcards
What does GPCR stand for?
G protein coupled receptor
Epinephrine is a derivative of _____
tyrosine
What are 3 components of heterotrimeric GPCR Signalling?
- plasma membrane receptor with 7 TM
- heterotrimeric guanosine nucleotide binding protein (G-protein)
- intracellular enzyme that generates a 2nd messenger
What does the binding of the ligand to the beta adrenergic receptor cause?
- structural change on cytoplasmic side
- G alpha,beta,gamma bind the B receptor
- Gprotein is GDP bound inactive
Gprotein bound to activated receptor causes:
- GDP/GTP exchange and binding affinity
- activated G protein = change shape = kick out the Ga-GTP
Gas - GTP associates with
Adenylyl cyclase
AC catalyzes the formation of
- ATP to form cAMP
cAMP activates
PKA
protein kinase a
which phosphorylates cellular proteins that cause a cellular response to epinephrine
Where can this beta adrenergic pathway be stopped?
- Gai (inactivate/inhibitory) binds and deactivates adenylyl cyclase (cant form cAMP)
- phosphodiesterase PDE breaks down cAMP to 5’AMP
What does caffeine do to this pathway?
- inhibits PDE
- prevents breakdown of cAMP
Gs bound GDP is ____
inactive
cannot activate AC
Gs contact with hormone receptor (beta adrenergic receptor) causes
GTP displaces GDP bound to Gs
Gs bound GTP _____
- dissociates into Gsa and Gsby subunits
Active complex of Gs protein is ___
Gsa - GTP
- activates adenylyl cyclase
What do Gai proteins do?
- inhibit the formation of second messenger
- via cytoplasmic facing enzyme AC