TABLE 1

Capacity of HPIs (IC50) to inhibit BCRP IC50 values (mean ± S.D., n = 3–4 independent experiments) were determined in the presence of a range of ritonavir, saquinavir, and nelfinavir concentrations (0–150 μM) as described under Materials and Methods.






IC50


Ritonavir Saquinavir Nelfinavir
μM
Wild-type, 482R 19.5 ± 0.8* 19.5 ± 6.7* 12.5 ± 4.1*
Mutant, 482T 40.4 ± 2.8 36.3 ± 7.2 31.1 ± 6.8
Mutant, 482G
43.1 ± 11.1
41.3 ± 6.4
26.7 ± 4.3
  • * The IC50 values for 482R are significantly different (p < 0.05) from 482T or 482G as calculated by Student's t test