Pharma 2

Question 1

What are the 3 GPCR subfamilies?

Answer 1

Family A- Rhosopsin-like group
Family B- Secretin receptor family
Family C- Venus fly trap

Question 2

Name four GPCR interacting proteins:

Answer 2

Heterotrimeric G proteins
RGSs
Kinases
Beta-arrestins

Question 3

Name two GPCR toxins:

Answer 3

Cholera

Pertussis toxin

Question 4

What are the effects of cholera?

Answer 4

Causes ADP ribosylation of GalphaS
Prevents GTP hydrolysis
Always acting adenylate cylase
Continuous production of cAMP which helps regulate fluid control
Enormous loss of fluids and electrolytes leading to death

Question 5

What are the effects of pertussis toxin?

Answer 5

Prevents ADP-ribosylation of Galphai
Prevents release of GDP
Permanently inactive
Prevents inhibition of adenylate cyclase
Continuous production of cAMP which helps regulate fluid control
Enormous loss of fluids and electrolytes leading to death

Question 6

What are RGS proteins and what do they do?

Answer 6

Regulator of G protein signalling proteins

Act as negative regulators of G-protein signalling

Question 7

Rapid desensitisation of GPCRs happens how?

Answer 7

Phosphorylation of C terminal tail
Beta arrestin binding to phosphorylated GPCRs and promoting uncoupling of G proteins
Receptor internalisation

Question 8

What is the process of permanent GPCR reduction?

Answer 8

Desensitisation
Sequestration
Recycling/Downregulation

Question 9

Where to GPCR agonists and antagonists bind to?

Answer 9

The orthosteric site

Allosteric modulators do not bind here

Question 10

Treatment for type 1 diabetes?

Answer 10

Islet transplantation
Insulin
Diet/exercise
Lifestyle

Question 11

Treatment for type 2 diabetes?

Answer 11

Diet/exercise

Lifestyle

Question 12

What do sulphonureas do?

Answer 12

Stimulate insulin secretion by:

• Binding to SUR1 receptor
• Depolarising membrane
• Opens VDCC
• Stimulates exocytosis of insulin

Side effects include hypoglycaemia and weight gain

Question 13

What do thiazidiones do?

Answer 13

Insulin sensitisers:

• Bind PPARgamma receptor
• PPARgamma complexes with the retinoid X receptor
• Enhances glucose sensitive genes like GLUT4
• Increase in glucose uptake

Question 14

What are the parts of the peripheral nervous system?

Answer 14

Somatic nervous system-skeletal muscle
Enteric nervous system-gut
Autonomic nervous system
-Sympathetic-fight or flight
-Parasympathetic-rest and digest

Question 15

What happens to neurotransmitters at a synapse?

Answer 15

1. Synthesis
2. Storage (package and protect)
3. Release
   - docking of vesicle
   - ca2+ entry
   - fusion
4. Activation
5. Inactivation