Chemical Transmission and Receptors Flashcards
Describe ionotropic receptors
Specific ligand activated
Directly alter ionic currents
Rapid response
Doesn’t amplify the signal
Describe metabotropic receptors
Indirectly alters ionic currents
Slower response
Amplify the signal
Describe receptor tyrosine kinases
Indirectly alters ionic currents by phosphorylating 2nd messengers or the receptor directly
Slower response
Amplify the signal
Describe G-protein coupled receptors (GPCRs)
Consists of 7 membrane spanning alpha helices
Guanin nucleotide-binding proteins termed G proteins
State the three subunits of GPCRs
Alpha
Beta
Gamma
Describe the resting state of GPCRs
Resting inactive state= GDP is bound to a subunit
Describe the ligand binding step of activation of GPCRs
Explain influence of GEFs and GAP
Ligand binding promotes a conformational change in heterotrimer and release of GDP and binding of GTP
Guanine exchange factor (GEFs) facilitates this exchange
GTPase (GTPase activating protein, GAP) is associated with g protein activation but cleavage to GDP leads to inactivation
Describe the stimulation step of GPCRs
GDP-GTP exchange stimulates dissociation of G Protein complex from receptor
GAP proteins involved in GPCRs
Regulation of G-protein signalling
Family of proteins that enhance some alpha subunits and GTPases activity
State properties of alpha and betagamma effector molecules
Alpha= water soluble
Betagamma= lipid associated