Molecular Basis of Drug Design

Question 1

Gene expression

Answer 1

amount of enzyme synthesised

Question 2

Feedback loop

Answer 2

very common regulatory mechanism, inhibition caused by product of the reaction or pathway

Question 3

Feed forward activation

Answer 3

product of a reaction activates a downstream enzyme, increasing substrate flow through the pathway

Question 4

Allosteric regulation

Answer 4

a regulator that binds to a site other than the active site. Alters activity through changes to the enzyme’s tertiary and quaternary structure

Question 5

Phosphorylation/Dephosphorylation

Answer 5

a common method in signal transduction, where addition/removal of a phosphate group can switch enzyme activity on or off

Question 6

Proteolysis

Answer 6

enzymes can be activated by proteolytic cleavage

Question 7

Phosphorylation - addition of phosphate group to…

and what is it important in?

Answer 7

Serine, Threonine, Tyrosine residues.

Very important in cell signalling events and cell cycle

Question 8

How does irreversible inhibitor work?

Answer 8

It reacts with the enzyme making it enzymatically inactive and the active enzyme cannot be regenerated

Question 9

How do irreversible inhibitors bind?

Answer 9

They bind covalently to the enzyme and cannot be removed

Question 10

How does reversible inhibition work?

Answer 10

They can bind to the enzyme and then be released leaving the enzyme in its original condition

Question 11

Name the types of reversible inhibition:

Answer 11

3 types:
1- Competitive
2- Non-competitive
3- Uncompetitive