Exam 4 - Stahelin nNRTIs (study)

Question 1

Describe how the nNRTIs inhibit RT.

Answer 1

Bind directly to site on RT but not in same spot as nucleotide. This changes the conformation of RT enough to inhibit nucleotide binding in its site.

Question 2

Describe where the nNRTIs bind to RT and what the consequences of binding are.

Answer 2

Bind in hydrophobic pocket near catalytic site.
Different site than NRTIs.
Do NOT compete with nucleotides for binding (they are non-competitive inhibitors)
Do NOT need to be phosphorylated.

Question 3

How does HIV become resistant to nNRTIs?

Answer 3

By mutations in the binding site of the nNRTIs.

Question 4

which nNRTI is potentially teratogenic?

Answer 4

efavirenz (1st gen)

Question 5

benefits of 2nd gen nNRTIs
Etravirine and Rilpivirine

Answer 5

Designed to be more flexible and able to bind in multiple orientations. Less likely for resistance mechanisms to inhibit them.

Question 6

Nevirapine SE

Answer 6

hepatotoxicity, rash (SJS)

Question 7

List the nNRTIs

Answer 7

1st gen:
-nevirapine
-efavirenz
-delavirdine
2nd gen:
-etravirine
-rilpivirine
long-acting inj.:
-cabotegravir
-rilpivirine