Lecture #1

Question 1

what is a ligand?

Answer 1

a molecule (biological or other) that interacts with another molecule

Question 2

what is a xenobiotic?

Answer 2

a molecule that is not present naturally in the human body but is synthesized - able to interact with a protein

Question 3

what does quality mean in terms of drug discovery?

Answer 3

means to populate the chemical space in terms of physical properties and to ensure the ideal pharmacokinetic profile

Question 4

what is pharmacokinetics?

Answer 4

the fate of the molecule within the body

Question 5

what is the objective of chemistry-driven drug discovery?

Answer 5

to design a molecule that is not only able to maximize the recognition of the binding site, but is also stable enough to survive a long time after the systemic administration and maximize its concentration at the site of action

Question 6

what does modern refer to?

Answer 6

implies there was an evolution from the past

Question 7

which is easier to do, create an effective drug or create a safe drug?

Answer 7

an effective drug

Question 8

on average how long does it take to create a drug and go through all the steps?

Answer 8

more than 12-13 years

Question 9

in 2017, what were the top 4 causes of death?

Answer 9

cardiovascular disease, cancer, respiratory disease, and diabetes

Question 10

what is Parkinson’s disease?

Answer 10

a slow progressive disease of the CNS due to a reduction in the amount of dopamine in specific areas of the brain (substantial nigra)

Question 10

what is Parkinson’s disease?

Answer 10

a slow progressive disease of the CNS due to a reduction in the amount of dopamine in specific areas of the brain (substantial nigra)

Question 11

what does Parkinson’s effect?

Answer 11

the motor system at the early stage of the disease, and at the late stage there is a clear impact in terms of depletion → it is a degenerative process responsible for the loss of the cognitive process

Question 12

what is a challenge when developing drugs for Parkinson’s?

Answer 12

the only drug at the moment has a tolerance mechanism occurring - there’s a need to increase the dose in order to maintain its effectiveness

Question 13

what is a glioblastoma?

Answer 13

one of the mot devastating brain tumors - available drugs have minimal efficacy and the median survival time is 15 months

Question 14

what is the main issue in terms of drug discovery when dealing with cancer?

Answer 14

the ability of chemotherapeutics to get across the blood brain barrier

Question 15

what happens in Duchenne muscular dystrophy?

Answer 15

muscles are progressively replaced by fibroadipogenic tissues and fibrotic tissues causing death at early stages

Question 16

what does chronic hepatitis B often evolve into?

Answer 16

liver disease, particularly hepatocarcinoma and cirrhosis

Question 17

what was the first tyrosine kinase inhibitor identified?

Answer 17

Ibrutinib