Roundup

Question 1

what are viral protease inhibitors

Answer 1

enzymes encoded in viral DNA or RNA
- catalyse cleavage of peptide bonds in viral polyprotein precursors

Question 2

what are viral protease inhibitors effective in

Answer 2

effect in HIV therapy
- ritonavir
- indinavir

Question 3

what are RNA dependent RNA polymerase inhibitors

Answer 3

interfere with synthesis of new viral RNA
- inhibit the reproduction of virus

Question 4

what are viral maturation inhibitors

Answer 4

Bind to a hIV protein precursor, preventing maturation
- inhibits formation of viable virus particles

Question 5

give an example of a viral maturation inhibitor

Answer 5

bevirimat

Question 6

what is involved in assay development

Answer 6

if the lead activity molecule is an enzyme inhibitor that works by binding to the enzyme itself
- obtain purified enzyme
- sequence homology (are there other similar enzymes)
- develop an assay (substrate, detection methods)

Question 7

what are the attributes of an ideal assay

Answer 7

1. simple- run without elaborate preparation or training
2. accurate- capable of meaningful quantification with a reasonable margin for activity
3. reproducible
4. selective
5. sensitive- detect very small amounts of activity
6. fast and economical

Question 8

what are the disadvantages in using whole animal assays for measuring activity of test molecules

Answer 8

• slow
• expensive
• risky
• complex

Question 9

what are the advantages and disadvantages in using whole cell bioassays for measuring activity of test molecules

Answer 9

• faster
• difficult to automate
• detection could be problematic

Question 10

what are the advantages of using isolated enzyme assays for measuring activity of test molecules

Answer 10

• rapid turnaround
• cheaper
• easier to automate
• detection can be easier to automate

Question 11

what do you need to know for formulation development

Answer 11

1. route of administration
2. formulation type
3. salt form
4. crystal form
5. water solubility