Receptors Flashcards
What effect does Vibrio cholera have on g-protein coupled receptors?
No deactivation of subunit.
What effect does Bordella pertussis (whooping cough)have on g-protein coupled receptors?
No activation.
Which type of receptor(s) activate cAMP production? B1AR, Alpha1AR, m2 AchR, m3AchR
B1AR- inc heart rate
Bronchodilation and
Which type of receptor(s) inactivate cAMP production? B1AR, Alpha1AR, m2 AchR, m3AchR
M2 AchR
Decreases heart rate and contraction
Which type of receptor(s) activate Ca++ and lipid signaling? B1AR, Alpha1AR, m2 AchR, m3AchR
Alpha1AR- Dec blood to skin, inc BP
m3AchR-Bronchoconstriction
What effect does caffine have on AMP
It decreases the amount of AMP because it inhibits the conversion of cAMP (second messanger) to AMP.
Which subunit of the G protein activates GIRK (K channel)? What effect on heartrate would an open GIRK have on the heart?
Beta-gamma subunit of the Gi of the M2AchR.
Decreased rate and decreased contraction.
What effect to B2-adrenergic receptors have on lung tissue?
Bronchodialation
Which receptor leads to bronchoconstriction in the lungs?
m3 AchR
Describe the process of desensitization of GPCRs
GRK (G receptor kinase) phosphorylates the g-protein and causes the Alpha subunit to dissociate. B-arrestin binds and dissociates the other subunits. The receptor is then endocytosed where it can be degraded or recycled
B-arrestin can also interact with MEK and ERK downstream.
The open conformation of a glycine loop in a Kinase is associated with which step of the reaction?
ATP/ADP exchange.
What are the major excitatory/inhibitory molecules in the CNS?
Glutamate=excitatory
GABA=Inhibitory
NMDA receptors are involved in learning. Describe the process by which NMDA receptors let calcium into the cell.
AMPA receptors next to the NMDA receptors bind glut and let Na+ in.
This depolarizes the membrane and results in the Mg++ ion that blocks NMDA to leave.
Calcium enters cell.
More AMPA receptors are recruited.
What does CYP 17 do? What inhibits it?
CYP 17 plays a role in androgen production.
Abiraterone inhibits CYP 17
What is enzalutamide?
Anti androgen receptor that treats prostate cancer by blocking AR nuclear entry, Ca Binding, and DNA binding
