TABLE 4.

Antiviral activity of test compounds against the wild type and an HIV-1 clone mutated in the LA loop of gp120 at several N glycosylation sites

Test compoundEC50 (μg/ml) fora:
Wild-type HIV-1bMutant HIV-1c (N200Q, N204Q, N211Q)
HHA0.23 ± 0.10≥4
GNA0.15 ± 0.07≥4
LOA0.28 ± 0.320.35 ± 0.07
Cyanovirin0.013 ± 0.0070.070 ± 0.014
AMD31000.011 ± 0.0060.045 ± 0.35
DS-50000.45 ± 0.071.75 ± 0.35
UC7810.002 ± 0.0010.003 ± 0.0
Tenofovir0.49 ± 0.202.0 ± 1.22
  • a EC50, compound concentration required to inhibit HIV-1-induced cytopathicity in CEM cell cultures by 50%. Data are the means of two to three independent experiments (± standard deviations). The wild-type and mutant (N200Q, N204Q, and N211Q) HIV-1 stocks contained 1,899 and 1,847 of p24/ml, respectively. The wild-type HIV-1 stocks contained 5,000 CCID50, whereas the mutant (N200Q, N204Q, and N211Q) stocks contained 350 CCID50. Therefore, the mutant HIV-1 clone has a ∼14-fold decreased infectivity compared to wild-type HIV-1 in CEM cell cultures.

  • b Wild-type HIV-1(BRU) clone.

  • c Mutant HIV-1(BRU) clone containing the N200Q, N204Q, and N211Q mutations in the hypervariable LA loop of gp120.