TABLE 4.
HIV-derived peptide inhibitors that interfere with HIV protein associations
| HIV protein association | Drug target(s) | HIV protein(s) (positions), sequence of HIV-derived peptide inhibitora | Mechanism(s) of drug action | Reference |
|---|---|---|---|---|
| RT-integrase | Integrase | RT (176–195), PDIVIYQYMDDLYVGSDLEI | RT-derived peptides inhibit 3′-end processing and the strand transfer reaction of integrase | 575 |
| Integrase | RT (366–385), KQLTEAVQKITTESIVIWGK | |||
| Integrase | RT (396–415), ETWETWWTEYWQATWIPEWE | |||
| RT | Integrase (46–65), KGEAMHGQVDCSPGIWQLDC | IN-derived peptide binds to RT and inhibits RT activity | 576 | |
| Vpr-integrase | Integrase, RT | Vpr (57–71), VEAIIRILQQLLFIH | Vpr-derived peptides inhibit activities of integrase and RT | 162 |
| Vpr-RT | Integrase, RT | Vpr (61–75), IRILQQLLFIHFRIG | ||
| Integrase-Rev | Integrase | Rev (13–23), FRKLIYLTKVL | Rev-derived peptides bind to integrase and inhibit enzymatic activities of HIV-1 integrase | 174 |
| Integrase | Rev (53–67), GLYRTSPSGRIWSI | |||
| Rev | Integrase (66–80), WTHLEGKIILVAVHVA | Integrase-derived peptides abrogate the inhibitory effect of Rev upon viral integration | 180 | |
| Rev | Integrase (118–128), WGSNFTSTTVKA | |||
| Protease-Vif | Protease | Vif (1–9), MENRWQVMI | The N-terminal domain of Vif inhibits the enzymatic activity of HIV-1 protease | 516 |
| Protease | Vif (21–65), WKSLVKHHMYVSGKARGWFYRHHYESPHPRISSEVHIPLGDARLV | 520 | ||
| Protease-p6* | Protease | p6* (65–68), SFNF | The C terminus of p6* inhibits HIV-1 protease activity | 508 |
| Protease | PR (1–5), Tat (49–61), p6* (65–68), PR (95–99), PQITLRKKRRQRRRPPQVSFNFATLNF | Inhibits protease dimerization and activities | 580 |
a
Peptide information begins with the HIV protein name followed by the peptide-derived region in the HIV protein and the peptide sequence. For instance, “RT (176–195), PDIVIYQYMDDLYVGSDLEI” shows a peptide with the sequence “PDIVIYQYMDDLYVGSDLEI,” which is derived from HIV RT between amino acid positions 176 and 195. Only representative peptide inhibitors with potent inhibitory activity were collected from the literature. Note that p6* is a transframe region in GagPol precursor proteins (Fig. 10).