TABLE 3.
Inhibition coefficients of HIV-1 protease mutant (M46I, G48V, I50V, I84L)a
Protease inhibitorb |
ki (nM) for:
|
Mutant/ wild-type ratio | |
---|---|---|---|
Wild type | Mutant | ||
APV | 0.6 | 1.3 | 2 |
SQV | 0.8 | 240 | 300 |
IDV | 1 | 4 | 4 |
RTV | 0.3 | 0.5 | 2 |
NFV | 1.1 | 1.4 | 1 |
For details, see reference 10. The substrate His-Lys-Ala-Arg-Val-Leu/p(NO2) Phe-Glu-Ala-Nle-Ser-NH2 is referred to as substrate 1 in reference 10. Assay conditions were as in the experiment in Table 2, except that the various PIs were allowed to preincubate with the wild-type or mutant protease and the reactions were initiated by addition of the substrate. Ki values were determined as described in the footnote to Table 2.
IDV, indinavir; RTV, ritonavir; NFV, nelfinavir.