Table 1

Mutations in HIV-1 integrase confer resistance to diketo acid inhibitors. ND, not determined; Und., undetermined.

Constructed mutationsStrand transfer (IC50, μM)HIV-1 infectivity (IC50, μM)
L-708,906L-731,988L-708,906L-731,988L-697,661*
WT HXB20.10.12.51.00.03
T66I0.60.68.07.0ND
S153Y0.60.2101.0ND
M154I0.50.55.04.0ND
T66I/S153YUnd. Und. >5010.00.04
T66I/M154I1.01.516.012.00.05
  • * Nonnucleoside inhibitor of HIV-1 reverse transcriptase (13).

  • Activity against the T66I/S153Y mutant could not be determined because of poor activity of the purified protein.