TABLE 1

Resistance profiles of HIV-1 mutants to diverse HIV-1 fusion inhibitors

HIV-1NL4-3 virus or mutantResistance to the indicated short-peptide fusion inhibitoraCross-resistance to the indicated large fusion inhibitorb
SC22EKMTSC22HP23T20SFTC34
IC50cFold changedIC50Fold changeIC50Fold changeIC50Fold changeIC50Fold changeIC50Fold change
Wild type50.25 ± 8.411.37 ± 0.4310.45 ± 0.16166.9 ± 0.1611.28 ± 0.3211.09 ± 0.121
L34S58.47 ± 2.021.121.69 ± 0.261.230.58 ± 0.081.29228.12 ± 51.53.412.55 ± 0.151.991.87 ± 0.331.72
D36G48.11 ± 5.820.961.4 ± 0.071.020.55 ± 0.151.222.11 ± 0.20.031.14 ± 0.340.890.6 ± 0.060.55
E49K1,098.67 ± 2.8921.8667.47 ± 10.1849.255.06 ± 0.6311.24197.5 ± 13.492.953.69 ± 0.482.883.11 ± 0.832.85
N126K126.7 ± 3.962.522.6 ± 0.091.91.43 ± 0.173.16236.9 ± 15.23.542.78 ± 0.162.173.19 ± 0.242.93
L34S/D36G85.84 ± 15.21.711.83 ± 0.561.341.01 ± 0.232.2438.13 ± 2.670.571.95 ± 0.261.521.81 ± 0.171.66
D36G/E49K1,032.37 ± 147.6320.5477.18 ± 4.4856.334.95 ± 0.4810.9510.8 ± 0.420.162.58 ± 0.362.021.95 ± 0.251.79
D36G/N126K131.1 ± 16.662.613.32 ± 0.662.421.33 ± 0.112.968.71 ± 1.960.132.66 ± 0.352.082.53 ± 0.192.32
E49K/N126K2,248.17 ± 240.0344.74150.5 ± 3.82109.8514.64 ± 0.5132.53204.2 ± 50.813.1514.78 ± 1.0311.5519.29 ± 1.0117.69
D36G/E49K/N26K1,414.67 ± 141.3628.15157.25 ± 19.77114.7814.68 ± 2.6332.6234.14 ± 2.580.5110.11 ± 0.577.910.6 ± 0.379.72
L34S/D36G/E49K635.89 ± 195.7612.6631.95 ± 2.923.323.79 ± 0.358.4223.5 ± 4.710.355.38 ± 0.464.22.75 ± 0.152.52
L34S/D36G/E49K/N126K2,598.33 ± 452.8151.71172.13 ± 19.88125.6421.72 ± 1.4748.2799.16 ± 59.421.6713.82 ± 1.6510.87.39 ± 2.776.78
L34S/D36G/E49K/E136G2,649.85 ± 154.3852.73177.28 ± 18.34129.435.58 ± 3.9179.07110.67 ± 11.751.6523.48 ± 1.4618.3418.86 ± 1.5717.3
  • a SC22EK and SC22EK-based short-peptide HIV-1 fusion inhibitors.

  • b T20 is a first-generation HIV-1 fusion inhibitor, SFT is a next-generation inhibitor, and C34 is a template peptide for SFT and many other inhibitors.

  • c IC50, 50% inhibitory concentration.

  • d Fold change in the IC50 was determined relative to the wild-type level.