Membrane Receptors Flashcards
Four main types of receptors
Ligand gated ion channels (Ionotropic receptors)
G protein coupled receptors
Kinase linked receptors
Nuclear receptors
What are G protein coupled receptors GPCRs
• Largest family of membrane receptors (~800)
• 7TM domain
• Mediate effects of many hormones and neurotransmitters
• Major targets of pharmacological intervention (~40% drugs on market)
What are the G protein subunits
Alpha
Beta
Gamma
How GPCRs inmate change
Signalling molecule binds to GPCRS and causes conformational change
Alpha subunit exchanges GDP for GTP
Alpha dissociates from beta and gamma
Alpha subunit regulates target proteins
GTP hydrolysed into GDP and ready to initiate another reaction
Different effects of G protein
Activate second messenger ATP to cAMP regulated by alpha subunit
Ion channels regulated by beta and gamma subunits
Effect of G alpha s unit
↑adenylyl cyclase
Effect of Gαi/o
↓ adenylyl cyclase
What is adenylyl cyclase activated by
Effector enzyme activated by Gαs