Table 2.
RT Inhibition with NNRTI and NNRTI/ HC-PGC nanoparticles.
| Test compound | HIV-1 reverse transcriptase | RNA-dependent DNA polymerization, IC50 (μM) | DNA-dependent DNA polymerization, IC50 (μM) | ||
|---|---|---|---|---|---|
| From DMSO stock solution | Complex with HC-PGC | From DMSO stock solution | Complex with HC-PGC | ||
| Z107 | Wild type | 3±1 | 5±1 | 0.7±0.2 | 0.5±0.1 |
| L100I | 10±3 | 15±4 | 3±1 | 1.5±0.2 | |
| K103N | 40±10 | 100±30 | 70±2 | 95±15 | |
| V106A | >100 | >100 | >100 | >100 | |
| Y181C | 5±2 | 40±10 | 6±2 | 1.9±0.5 | |
| G190A | 35±10 | 70±20 | 45±15 | 0.9±0.3 | |
| K103N+Y181C | 80±30 | 100±20 | 50±20 | 9±2 | |
| Z011 | Wild type | - | - | 0.7±0.1 | 1.2±0.4 |
| L100I | - | - | 1.8±0.6 | >100 | |
| K103N | - | - | 6±1 | >100 | |
| V106A | - | - | >100 | >100 | |
| Y181C | - | - | 1.4±0.5 | 22±5 | |
| G190A | - | - | 1.6±0.3 | 2.6±0.7 | |
| K103N+Y181C | - | - | 10±3 | >100 | |
| Z007 | Wild type | 50±20 | 100±20 | 40±10 | 8±2 |
| L100I | 100±30 | >100 | >100 | >100 | |
| K103N | >100 | >100 | >100 | >100 | |
| V106A | >100 | >100 | >100 | >100 | |
| Y181C | >100 | >100 | >100 | >100 | |
| G190A | >100 | >100 | >100 | >100 | |
| K103N+Y181C | >100 | >100 | >100 | >100 | |