Challenges In Drug Optimisation

Question 1

What are the challenges in coming up with new drug ideas?

Answer 1

*body highly complex- several messengers, receptors, enzymes eg many receptors and enzymes can be targeted to treat hypertension
*often, more than one target may need to be addressed
*drugs designed against specific target may become less effective over time- blockade could be bypassed

Question 2

What is lipinskis rule of five and what does it mean?

Answer 2

Important to make drug orally active
*MW <500
*logP<5 (partition coefficient)
*less than 10 H bond acceptors
*less than 5 H bond donors

Question 3

What is a pharmacophore?

Answer 3

Section of ligand that binds to a receptor and exerts physiological response

Question 4

What 5 properties should be considered in drug discovery?

Answer 4

*potency
*selectivity
*structural novelty
*solubility
*chemical/plasma stability