Table 1.
Sequence of the substrate analog inhibitors and inhibition constants. Values are listed for Ki, in μm, and values in parenthesis are the Ki relative to PR. PR, wild type HIV-1 protease; PRV82A, PR with the V82A mutation; PRI84V, PR with the I84V mutation.
| Cleavage site | Peptide sequence | PR | PRV82A | PRI84V |
|---|---|---|---|---|
| CA-p2 | R-V-L-r-F-E-A-Nle | 0.075 ± 0.009 | 0.024 ± 0.004 (0.3) | 0.275 ± 0.031 (3.7) |
| p2-NC | Ace-T-I-Nle-r-Nle-Q-R | 2.17 ± 0.28 | 0.53 ± 0.078 (0.24) | 13.0 ± 1.5 (6.0) |
| p6pol-PR | V-S-F-N-F-r-P-Q-I-T-K-K | 22.1 ± 2.8 | 36.3 ± 5.4 (1.6) | 46.6 ± 5.3 (2.1) |
| p1-p6 | R-P-G-N-F-r-L-Q-S-R-P | 96.7 ± 12.3 | 28.2 ± 4.2 (0.3) | > 500 (> 5) |
| NC-p1 | E-R-Q-A-N-r-F-L-G-K-I | > 500 | > 500 | > 500 |