Table 4.
Activity of inhibitor 2 against HIV‐1 clinical isolates in PHA‐PBMCs.
|
Virus[a] |
IC50 values [μm] |
|||||
|---|---|---|---|---|---|---|
|
SQV |
APV |
IDV |
NFV |
RTV |
DRV (2) |
|
|
HIV‐1ERS104pre (wt X4) |
0.010 |
0.023 |
0.018 |
0.019 |
0.027 |
0.003 |
|
HIV‐1MOKW (wt R5) |
0.004 |
0.011 |
0.018 |
0.033 |
0.032 |
0.003 |
|
HIV‐1TM (MDR X4) |
0.23 (23) |
0.39 |
>1 (>56) |
0.54 (28) |
>1 (>37) |
0.004 (1) |
|
HIV‐1MM (MDR R5) |
0.30 (30) |
0.34 |
>1 (>56) |
>1 (>53) |
>1 (>37) |
0.02 (7) |
|
HIV‐1JSL (MDR R5) |
0.35 (35) |
0.75 (33) |
>1 (>56) |
>1 (>53) |
>1 (>37) |
0.029 (10) |
|
HIV‐1A (MDR X4) |
0.14 (14) |
0.16 (7) |
>1 (>56) |
0.36 (19) |
>1 (>37) |
0.004 (1) |
|
HIV‐1B (MDR X4) |
0.31 (31) |
0.34 (15) |
>1 (>56) |
>1 (>53) |
>1 (>37) |
0.013 (4) |
|
HIV‐1C (MDR X4) |
0.037 (4) |
0.28 (12) |
>1 (>56) |
0.44 (23) |
>1 (>37) |
0.003 (1) |
|
HIV‐1G (MDR X4) |
0.029 (3) |
0.25 (11) |
0.39 (22) |
0.32 (17) |
0.44 (16) |
0.004 (1) |
[a] Amino acid substitutions identified in the protease‐encoding regions of viruses compared to the consensus sequence cited from the Los Alamos database. See reference 105 for details.