9. Signalling between cells II Flashcards
Describe Ionotropic receptor signal transduction events
- Ligand binds to the receptor protein
- Change in conformation of channel protein: opens pore
- Pore allows ions to move in or out of cell according to their respective concentration gradients
Give 2 examples of ionotropic receptors.
Nicotinic Acetylcholine Receptor
GABAA Receptor
Describe the Nicotinic Acetylcholine Receptor
Ligand: Acetylcholine (ACh)
Location: Skeletal muscle
Physiological effect: Muscle contraction
Describe the GABAA receptor
Ligand: gamma-amino butyric acid (GABA)
Location: Neuronal
Physiological effect: decrease neuronal excitability
Describe the activation process of a G-protein coupled receptor
Ligand binds and changes conformation of the receptor
Unassocciated G protein binds to the intracellular part of receptor (it has a GDP bound to it)
GDP is exchanged for GTP
GTP allows the dissociation of the alpha subunit and the beta-gamma subunit of the G protein
Subunits bind to target proteins
Once the alpha subunit has fulfilled its function, GTPase activity on dephosphorylates GTP to GDP
Allows alpha subunit to dissociate from target protein and reform the heterotrimer with GDP attached
What is a G-protein coupled receptor?
Heterotrimeric of alpha, beta and gamma chains with a GDP attached
What are the 3 types of G alpha subunits?
G alpha S
G alpha I
G alpha Q
What is the function of G alpha S?
Stimulates adenyl cyclase
Converts ATP to cAMP
cAMP activates PKA
Give an example of action of G alpha S
Beta-1- adrenergic receptor in sympathetic nervous system
Increases heart rate and force of contraction
What is the function of G alpha I?
Inhibits adenylyl cyclase
Thus, reduces levels of PKA
Give an example of action of G alpha I
M-2- muscarinic receptor in parasympathetic nervous system
Decreases heart rate
What is the function of G alpha Q?
Stimulates phospholipase C (PLC) Converts PIP2 to IP3 and DAG IP3 stimulates Ca2+ release DAG activates PKC Important in smooth muscle contraction and vasoconstriction
Give an example of action of G alpha Q
AT-1 angiotensin receptor
Causes vasoconstriction
Describe the action of enzyme-linked receptors.
Ligand binds to the receptors, causes receptor clustering
Clustering of receptors activates intracellular enzymes,
Enzymes phosphorylate receptor which leads to binding of signalling proteins to cytoplasmic domain
Signalling proteins recruit other signalling proteins, generate a signal
What are the 3 types of enzyme-linked receptor?
Tyrosine Kinase (95%)
Guanylyl-Cyclase
Serine-Threonine Kinase