TABLE 4.
Compound | Mean EC50 ± SD (nM) for wt | Mean change (fold) in EC50 ± SDb
|
|||||||
---|---|---|---|---|---|---|---|---|---|
M184V | V118I-M184V | M41L-V118I- M184V | A62T-V118I-M184V | M41L-S68N-G112S-M184V | M41L-A62V- S68N-G112S-M184V | M41L-A62V-S68N-G112S-V118I-M184V | G112S-M184V | ||
VRX-329747 | 176.9 ± 1.6 | 3.5 ± 1.0* | 3.3 ± 0.6* | 6.5 ± 1.6* | 6.3 ± 1.0* | 10.3 ± 0.4* | Max* | 34.7 ± 18.6* | ND |
VRX-413638 | 45.1 ± 0.5 | 3.9 ± 0.3* | 4.2 ± 0.8* | 9.8 ± 0.6* | 9.5 ± 4.2* | 36.5 ± 3.0* | Max* | Max* | ND |
Efavirenz | 0.7 ± 0.1 | 0.7 ± 0.02 | 0.6 ± 0.01 | 0.6 ± 0.01 | 0.5 ± 0.05 | 0.2 ± 0.02 | 0.3 ± 0.02 | 0.2 ± 0.002 | ND |
AZT | 60.8 ± 1.2 | 0.5 ± 0.05 | 0.4 ± 0.07 | 0.4 ± 0.04 | 0.5 ± 0.02 | 0.1 ± 0.01 | 0.1 ± 0.02 | 0.1 ± 0.03 | ND |
ddI | 2,636.5 ± 841 | 2.4 ± 0.4 | 2.2 ± 0.9 | 1.7 ± 0.2 | 1.9 ± 0.9 | 1.4 ± 0.5 | 0.3 ± 0.2 | 0.7 ± 0.2 | ND |
d4T | 1,221.0 ± 255 | 1.3 ± 0.2 | 1.3 ± 0.3 | 1.1 ± 0.3 | 1.1 ± 0.1 | 0.6 ± 0.2 | 0.4 ± 0.02 | 0.4 ± 0.1 | ND |
Abacavir | 1,647.5 ± 126 | 4.7 ± 1.4* | 4.9 ± 1.0* | 2.6 ± 0.3* | 3.0 ± 0.7* | 1.4 ± 0.1 | 0.6 ± 0.2 | 0.7 ± 0.2 | ND |
Tenofovir | 555.5 ± 122 | 1.0 ± 0.3 | 1.0 ± 0.04 | 1.0 ± 0.3 | 1.1 ± 0.1 | 0.5 ± 0.1 | 0.5 ± 0.3 | 0.4 ± 0.1 | ND |
FTC | 76.7 ± 7.9 | Max* | Max* | Max* | Max* | Max* | Max* | Max* | ND |
% wt RCc | 100 | 85.2 ± 7.9 | 119.9 ± 11.1 | 81.8 ± 4.7 | 121.6 ± 12.6 | 143.8 ± 10.2 | 15.9 ± 1.1 | 105.9 ± 12.1 | 0.2 ± 0.04 |
Molecular clones were built in the reporter vector pNL4-3.Luc.R−E, and EC50 values were determined using HeLa-JC-53 cells.
Mean EC50 values ± SD were from two tests. Max, could not be determined because the EC50 was >10 μM; ND, not determined because of the poor replication capacity of the virus. *, EC50 was statistically significantly higher than that against wild-type virus (P < 0.05).
Virus replication capacity was determined in the absence of inhibitor.