HIV therapy Flashcards
What does NRTI stand for?
Nucleoside analogue reverse transcriptase inhibitors
Examples of NRTIs
AZT, ddl and ddC
What does NNRTI stand for
Non-nucleoside reverse transcriptase inhibtors
Example of a protease inhibitor
Squinavir
What does HAART stand for
High active retroviral therapy
What does HAART consist of
2 NRTIs and + NNRTI/PI
What is PI
Protease inhibitor
What do NRTI/NNRTI block
Reverse transcription
What do PI inhibit?
MAturation
What is the structure of HIV-1 RT?
Heterodimer of P66 and P51, has RNAse and DNA pol activity
Are NRTIs selective or non-selective inhibitors?
Selective
What do NRTIs get phsophrylated by?
Cellular kinases
Do NRTIs bind to RT better than TTP?
Yes
How does NRTIs work?
Act as chain terminator, no 3’ OH group
What does AZT stand for?
Aziodythymidine
What was AZT first used as?
Anti-tumour agent
What two lentiviruses does AZT hibit?
MLV and HIV
Why is AZT used in combination therapy?
To avoid resistance
Example of NNRTIs
Nevirapine
How do protease inhibitors work?
Inhibit cleavage of Gag and Gag-Pol into individual polypeptides?
Side effect of protease inhibitors?
Lipodystrophy
What receptor does Maraviroc target?
CCR5 (antagnoist), for those infected with R5 virus.
What is Enfuvirtide marked as Fuzeon?
Peptide base entry inhibitor
How does enfuvirtide work?
Binds to a region of gp41 and disrupts the conformational changes associated with virus–host-cell fusion
What are capsid binding compounds based on?
Capsid binding proteins like TRIM5-alpha
Where does lenacapvir bind in HIV?
Pocket between capsid hexamers, prevents capsid dissociation
Examplse of integrase inhibitors
- Raltegravir
- Elvitegravir
- Doltegravir
What is PrEP
Pre-exposure prophylaxis
What is PEP
Post-exposure prophylaxis
Is PrEP an NRTI or NNRTI
NRTI
