TABLE 2.
Resistance profiles of diverse HIV fusion inhibitorsa
Pseudovirus |
LP-52 |
T20 |
LP-80 |
LP-83 |
LP-19 |
|||||
---|---|---|---|---|---|---|---|---|---|---|
EC50 (nM) | FC | EC50 (nM) | FC | EC50 (nM) | FC | EC50 (nM) | FC | EC50 (nM) | FC | |
SIVmac239 | ||||||||||
WT | 0.09 ± 0.01 | 1 | 394.55 ± 22.56 | 1 | 0.03 ± 0.001 | 1 | 0.002 ± 0.000 | 1 | 0.38 ± 0.03 | 1 |
F346L | 0.08 ± 0.03 | 0.94 | 400.58 ± 30.16 | 1.02 | 0.03 ± 0.004 | 1.09 | 0.002 ± 0.000 | 1 | 0.38 ± 0.02 | 0.99 |
V562A | 27.59 ± 3.31 | 324.6 | 23832.66 ± 1590.59 | 60.4 | 1.83 ± 0.43 | 70.19 | 0.025 ± 0.002 | 12.67 | 0.33 ± 0.03 | 0.86 |
V562M | 2.69 ± 0.41 | 31.65 | 3188.33 ± 775.16 | 8.08 | 0.38 ± 0.05 | 14.46 | 0.013 ± 0.001 | 6.5 | 0.25 ± 0.01 | 0.67 |
E657G | 0.44 ± 0.2 | 5.12 | 811.77 ± 228.22 | 2.06 | 0.17 ± 0.01 | 6.5 | 0.006 ± 0.001 | 3.17 | 1.35 ± 0.26 | 3.55 |
S760G | 0.07 ± 0.02 | 0.76 | 339.27 ± 74.99 | 0.86 | 0.03 ± 0.01 | 1.1 | 0.002 ± 0.001 | 0.83 | 0.36 ± 0.03 | 0.94 |
V562A/E657G | 403.5 ± 76.27 | 4747 | 21548.56 ± 2143.45 | 54.62 | 108.78 ± 6.61 | 4184 | 0.696 ± 0.140 | 348 | 1.24 ± 0.22 | 3.27 |
V562M/E657G | 34.12 ± 14.1 | 401.4 | 5344.44 ± 872.17 | 13.55 | 3.19 ± 0.49 | 122.5 | 0.09 ± 0.004 | 45.17 | 0.73 ± 0.05 | 1.92 |
V562A/S760G | 20.93 ± 5.49 | 246.2 | 12122.89 ± 2895.06 | 30.73 | 1.03 ± 0.09 | 39.65 | 0.031 ± 0.006 | 15.33 | 0.36 ± 0.03 | 0.95 |
V562M/S760G | 3.31 ± 0.89 | 38.94 | 2795.22 ± 370.75 | 7.08 | 0.31 ± 0.05 | 11.76 | 0.014 ± 0.004 | 6.83 | 0.21 ± 0.01 | 0.56 |
E657G/S760G | 0.38 ± 0.17 | 4.47 | 899.03 ± 92.97 | 2.28 | 0.13 ± 0.03 | 4.82 | 0.006 ± 0.001 | 3 | 1.06 ± 0.09 | 2.78 |
HIV-1 NL4-3 | ||||||||||
WT | 0.01 ± 0.002 | 1 | 103.18 ± 2.49 | 1 | 0.004 ± 0.001 | 1 | 0.002 ± 0.000 | 1 | 0.14 ± 0.02 | 1 |
V547A | 0.27 ± 0.03 | 42.26 | 1577.78 ± 204.37 | 15.29 | 0.25 ± 0.06 | 62 | 0.016 ± 0.001 | 8 | 0.16 ± 0.003 | 1.16 |
V547M | 0.15 ± 0.02 | 23.16 | 537.26 ± 58.61 | 5.21 | 0.12 ± 0.02 | 31 | 0.008 ± 0.001 | 4 | 0.21 ± 0.01 | 1.49 |
E646G | 0.01 ± 0.002 | 1.84 | 125.97 ± 9.46 | 1.22 | 0.01 ± 0.004 | 3 | 0.001 ± 0.000 | 0.5 | 0.17 ± 0.02 | 1.24 |
V547A/E646G | 0.71 ± 0.15 | 111.6 | 1519.33 ± 164.57 | 14.73 | 0.67 ± 0.1 | 167.8 | 0.043 ± 0.016 | 21.5 | 0.17 ± 0.03 | 1.23 |
V547M/E646G | 0.39 ± 0.04 | 62.11 | 660 ± 56.7 | 6.4 | 0.26 ± 0.08 | 65.75 | 0.011 ± 0.004 | 5.5 | 0.2 ± 0.06 | 1.44 |
Data were derived from three independent experiments and express as means ± standard deviations; FC, fold change; EC50, 50% effective concentration.