Drug Targets

Question 1

Most drugs are in equilibrium between…..

Answer 1

Bound and unbound states

Question 2

Drug size in comparison to target

Answer 2

Drug is smaller

Question 3

What are binding sites

Answer 3

Pockets on macromolecule

Question 4

What are receptors

Answer 4

Membrane bound particles that act as a relay to pass information to a secondary messenger

Question 5

What are agonists

Answer 5

Mimic the Natural ligands and activate exceptions - bring about induced fit

The 1st messengers which activates the 2ndary messenger via binding to a receptor and causing a conformational change

Unlike enzymes they are unchanged by binding

Question 6

Induced fit

Answer 6

Binding site changes shape to accommodate the messenger

Knock on effect causing the whole protein to change shape

Question 7

Antagonists

Answer 7

Block receptors and dont activate them - no induced fit

Question 8

Paul ehrlich side chin theory

Answer 8

1897

Drug Design

“The objective of the medicinal chemist in his/her quest for better medicinal compounds is to discover:
* which functional groups within a structure are important for its pharmacological activity
* how these groups can be modified to produce more potent, selective and safer compounds”

This is just as relevant now as it was in 1897. This method of drug design is what we’ll cover in the remainder of these sessions