C4 The biology of dyspepsia 4: Therapeutics

Question 1

What are the 3 ways an enzyme can bind to its target?

Answer 1

competitive inhibition - reversible binding in the active site
covalent modification
allosteric inhibition - at site distant from active site

Question 2

Where is carbonic anhydrase present?

Answer 2

tissues, including eyes, stomach, kidney, liver and brain

Question 3

Why is C. anhydrase needed?

Answer 3

secretion of HCl by parietal cells

Question 4

What is CA 2 used to treat?

Answer 4

glaucoma

Question 5

NSAIDs target which two enzymes?

Answer 5

COX -1 constitutive causes ADR

COX 2 - inducible, anti inflammatory/ pain relief

Question 6

Where is COX found?

Answer 6

attached to membrane of endoplasmic reticulum

Question 7

How do NSAIDs inhibit COX -1 & COX -2?

Answer 7

preventing binding of arachidonic acid

Question 8

Which COX enzyme has a desirable effect from NSAIDs?

Answer 8

COX -1 undesirable inhibition

COX -2 desirable

Question 9

Why does it take time for PPIs to work?

Answer 9

Proton pump in xytoplasmic vesicles not targeted by PPIs

recycling of proton pumps from c. vesicle to apical membrane required for full inhibition of all P.pumps