Lecture 31

Question 1

Imatinib targets a ____ protein, in cancer cells.

Answer 1

Imatinib targets a fusion protein

but has off-target effects

Question 2

what determines binding forces

Answer 2

The different types of bonds have different strength and range

e.g

Ion-ion
ion-dipole
hydrogen

Question 3

What are the two parts of a drug that confer affinity

Answer 3

Shape and its electronic features

Question 4

Affinity is…..

Answer 4

the likelihood of binding in the “pockets” of receptors

Question 5

Mass action states that….

Answer 5

The rate of chemical reaction is proportional to the concentration of the reactants

Question 6

At equilibrium, the receptor/drug system is ________, meaning there is space for an antagonist to compete with an agonist

Answer 6

At equilibrium, the receptor/drug system is dynamic, meaning there is space for an antagonist to compete with an agonist

Question 7

K (A) is the ________ ________constant

It represents the affinity. The concentration of drug at which _____the receptors will be occupied

Answer 7

K (A) is the equilibrium dissociation constant

It represents the affinity. The conc. of drug at which half the receptors will be occupied

Question 8

If you increase drug concentration, the forward rate will be ______

Answer 8

If you increase drug concentration, the forward rate will be faster

Question 9

If you reduce affinity, the receptor occupancy curve shifts to the _____.

Therefore higher concentration of drug is needed to occupy half of the receptors

Answer 9

If you reduce affinity, the receptor occupancy curve shifts to the Right.

Therefore higher con.c of drug is needed to occupy half of the receptors

Question 10

The negative log of the K (A) gets _______when the drug has a higher affinity.

Answer 10

The negative log of the K (A) gets bigger when the drug has a higher affinity.

Question 11

EC 50 is the….

Answer 11

EC 50 - is the concentration causing 50% of the maximal effect of the agonist on a particular tissue