3 - G-Proteins + Calcium Flashcards
How can you turn off a G-Protein?
GTPase in alpha subunit. Prevents overreactive. Drugs and toxins can target GTPase
How would you describe a G-protein?
What is the main set up of a GPCR?
- A receptor (ligand bind in TMD or N terminal)
- G-protein
- Effector (enzyme/ion channel)
- Second messenger
What are the three types of G-protein and what do they govern?
- Gs - Stimulate adenylate cyclase
- Gi - Inhibit adenylate cyclase
- Gq - Stimulate phospholipase C
What types of G-protein are all the main receptors?
M2 also salivary glands
What is the cascade pathway of a Gs protein?
What is the cascade pathway of a Gq protein?
How does a cholera and pertussis toxin work?
Pertussis - Gi protein. Covalently binds to alpha subunit and inhibits GDP exchange for GTP
Cholera - Prevents GTPase action so Gs-protein constantly activated, can lead to loss of Cl- from cells, leading to diarrheoa
What is the cascade pathway of a Gi protein?
How does Phospholipase C work?
- Cuts PIP2, (membrane phospholipid), into DAG and IP3.
- IP3: Water soluble so binds to LGIC on ER. Receptor stimulated and opens. Influx of calcium ions into cytosol
- DAG: Lipid soluble. Activates PKC, which acts on lots of proteins
How does cyclic AMP activate PKA?
PKA has 4 subunits. cAMP binds to R subunits and releases C subunits so they are active
How does positive inotropy in the heart work?
- B1 Adrenoreceptor therefore GS
- Sympathetic adrenaline
- PKA phosphorylates VOCC so that when there is wave of depolarisation, more Ca2+ enters the cell, more Ca2+ released from ER, more forceful contraction
What G protein is involved in smooth muscle contraction?
Q
- Vasoconstriction - a1
- Bronchoconstriction - M3
- GI Tract - a2?
How does arteriolar vasoconstriction work?
- Sympathetic noradrenaline on a1 receptors
- IP3 produced which releases Ca2+ from ER, leading to contraction
- DAG produced activates PKC which can activate proteins that sustain contraction
How do you modulate neurotransmitter release?
- U-opiod Gi receptor
- BY unit binds to VOCC stopping it from opening
- Less Ca2+ in cell, therefore vesicles containing neurotransmitter cannot be released