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Which class of antiretroviral drugs acts by blocking the insertion of viral DNA into the host genome in HIV infection?
- A Non-nucleoside reverse transcriptase inhibitors You picked ✕
- B Integrase strand transfer inhibitors You picked ✓
- C Entry inhibitors You picked ✕
- D Nucleoside reverse transcriptase inhibitors You picked ✕
- E Protease inhibitors You picked ✕
Correct!
Incorrect
The answer is B: Integrase strand transfer inhibitors
Explanation
Why B is correct
See HIV Antiretroviral Therapy. Option B is correct. HIV is a retrovirus: it carries its genes as RNA and uses its own enzyme, reverse transcriptase, to copy the RNA into DNA. The viral enzyme integrase then inserts this DNA into the host cell's own DNA. This integration step makes the infection permanent, because the viral genes are then copied along with the cell's own. Integrase strand transfer inhibitors (INSTIs) such as dolutegravir, raltegravir and bictegravir block integrase and stop this insertion. They are increasingly used as first-line treatment because of high efficacy and good tolerability, usually with two nucleoside reverse transcriptase inhibitors. A useful way to learn the classes is to follow the life cycle in order, with one class for each stage:
- Entry inhibitors (such as maraviroc) block attachment and entry into the cell
- NRTIs and NNRTIs block reverse transcriptase, which copies RNA into DNA
- Integrase inhibitors (dolutegravir, raltegravir, bictegravir) block insertion into the host genome
- Protease inhibitors (such as darunavir) block the maturation of viral proteins
- Integrase: The viral enzyme that inserts viral DNA into the host cell's DNA, which makes the infection permanent.
- INSTIs: Dolutegravir, raltegravir and bictegravir block integrase and stop this insertion.
- First-line use: Chosen for high efficacy and good tolerability, usually with two nucleoside reverse transcriptase inhibitors.
Why the other options are incorrect
- A. Non-nucleoside reverse transcriptase inhibitors: Non-nucleoside reverse transcriptase inhibitors also act at the reverse transcription step, by binding the enzyme directly. They act before integration, not at it. Your answer
- C. Entry inhibitors: Entry inhibitors act at the very first stage, by blocking attachment or entry through the receptors on the CD4 cell. They work before the viral DNA exists, so they cannot block integration. Your answer
- D. Nucleoside reverse transcriptase inhibitors: Nucleoside reverse transcriptase inhibitors act earlier, by blocking the copying of viral RNA into DNA. They are the backbone of most regimens but do not stop integration. Your answer
- E. Protease inhibitors: Protease inhibitors act late in the life cycle, by blocking the cutting of viral proteins so that new virus particles are immature. They come after integration, not at it. Your answer
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