TABLE 5.
Effects of human serum proteins on anti-HIV-1 activity of UIC-94017a
| Drug | 15% FCS
|
10 μM AAG
|
45% human serum
|
|||
|---|---|---|---|---|---|---|
| IC50 (μM) | IC90 (μM) | IC50 (μM) | IC90 (μM) | IC50 (μM) | IC90 (μM) | |
| UIC-94017 | 0.003 ± 0.0003 | 0.009 ± 0.0005 | 0.042 ± 0.011 (14) | 0.17 ± 0.10 (19) | 0.034 ± 0.0005 (11) | 0.11 ± 0.03 (12) |
| SQV | 0.010 ± 0.004 | 0.060 ± 0.008 | 0.033 ± 0.0006 (3) | 0.09 ± 0.002 (2) | 0.17 ± 0.12 (17) | 0.89 ± 0.13 (15) |
| APV | 0.023 ± 0.006 | 0.083 ± 0.004 | 0.35 ± 0.06 (15) | >1 (>12) | 0.35 ± 0.07 (15) | >1 (>12) |
| IDV | 0.018 ± 0.004 | 0.075 ± 0.002 | 0.051 ± 0.002 (3) | 0.35 ± 0.16 (5) | 0.069 ± 0.008 (4) | 0.61 ± 0.04 (8) |
| NFV | 0.019 ± 0.002 | 0.075 ± 0.0007 | 0.31 ± 0.01 (16) | 0.83 ± 0.01 (11) | 0.94 ± 0.06 (49) | >1 (>13) |
| RTV | 0.027 ± 0.009 | 0.082 ± 0.005 | 0.21 ± 0.16 (8) | 0.69 ± 0.19 (8) | 0.33 ± 0.05 (12) | >1 (>12) |
a
The IC50s and IC90s were determined by using PHA-PBMCs as target cells and the inhibition of p24 Gag protein production as an endpoint. All assays were conducted in triplicate. The results shown are means ± standard deviations from three independent assays. Numbers in parentheses represent fold increases in IC50 and IC90s in the presence of 10 μM AAG or 45% human serum compared to those determined in the presence of 15% FCS. The virus used was HIV-1ERS104pre.