TABLE 1.
Literature review and measured changes of integrant and two-LTR circle/episome levels in infected cells following interference with lentiviral integration
| Mode of IN interferencea | Cell type | Virus | Integrant fold reduction | Two-LTR circle/episome fold change | Reference |
|---|---|---|---|---|---|
| L-731,988 | 293T | HIV-1NL4-3 | >35 | Unchangedc | 7 |
| L-708,906 | 293T | HIV-1NL4-3 | >35 | Unchangedc | 7 |
| L-731,988 | T cells | HIV-1HXB2 | >300 | Unchangedc | 54 |
| L-731,988 | T cells | HIV-1HXB2 | >300 | 4 down | 54 |
| L-731,988 | CD4+ T cells | HIV-1NL4-3 | NAb | 4.3 up | 16 |
| L-708,906 | 293T | HIV-1NL4-3 | NAb | 10 up | 52 |
| Raltegravir | HeLa | HIV-1YU-2 | NAd | 3 up | This study |
| GSK501015 | HeLa | HIV-1YU-2 | NAd | Unchangedc | This study |
| Raltegravir | Rat2 | HIV-1YU-2 | NAd | 4 up | This study |
| GSK501015 | Rat2 | HIV-1YU-2 | NAd | 5 up | This study |
| IN D66V/D118A | CrFK | FIV | NAb | Unchangedc-2.6 up | 47 |
| IN D116N | CD4+ T cells | HIV-1NL4-3 | NAb | 3.5 up | 16 |
| IN D116N | SupT1 | HIV-1NL4-3 | NAb | 10 up | 26 |
a
Integration interference was achieved by INIs (top 10 rows) or catalytic site mutants of integrase (IN) (bottom 3 rows).
b
Not applicable; inhibition of integration was confirmed indirectly by viral-gene expression reporter assays or HIV p24CA immunofluorescence.
c
“Unchanged” was defined as an alteration of ≤2-fold.
d
Not applicable; inhibition of integration was indirectly validated by p24CA antigen enzyme-linked immunosorbent assay. Levels of p24CA in culture supernatants of INI-treated cells were ≥80% reduced compared to dimethyl sulfoxide-treated controls (n = 2 to 3).