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. 2018 Mar 6;9(2):e02425-17. doi: 10.1128/mBio.02425-17

TABLE 1 .

Antiviral activity of DRV against HIV-1 clones carrying various mutations in protease

Infectious clone Amino acid substitution(s) in PR IC50 (mean ± SD) (nM) (fold change)a
DRV APVb AZTc RALd
rHIVWT None 3.1 ± 0.3 24 ± 2 30 ± 9 4.9 ± 3.2
rHIVDRVRP51I32V L10I, I15V, K20R, L24I, L33F, M36I, M46L, I54M, L63P,
K70Q, V82I, I84V, L89M
29 ± 8 (9) ND ND ND
rHIVDRVRP51F33L L10I, I15V, K20R, L24I, V32I, M36I, M46L, I54M, L63P,
K70Q, V82I, I84V, L89M
120 ± 33 (38) ND ND ND
rHIVDRVRP51M54I L10I, I15V, K20R, L24I, V32I, L33F, M36I, M46L, L63P,
K70Q, V82I, I84V, L89M
43 ± 15 (14) ND ND ND
rHIVDRVRP51V84I L10I, I15V, K20R, L24I, V32I, L33F, M36I, M46L, I54M,
L63P, K70Q, V82I, L89M
28 ± 6 (9) ND ND ND
rHIVDRVRP51 L10I, I15V, K20R, L24I, V32I, L33F, M36I, M46L, I54M,
L63P, K70Q, V82I, I84V, L89M
330 ± 10 (106) ND ND ND
rHIVV32I/L33F/I54M/I84V V32I, L33F, I54M, I84V 639 ± 17 (205) ND ND ND
rHIVV32I V32I 0.2 ± 0.05 (0.06) 31 ± 3 (1.3) 32 ± 6 (1.1) 4.7 ± 0.5 (1.0)
rHIVL33F L33F 3.2 ± 0.1 (1.0) 35 ± 2 (1.3) 45 ± 12 (1.5) 5.6 ± 1.1 (1.1)
rHIVI54M I54M 2.7 ± 0.1 (0.9) 324 ± 86 (13) 34 ± 17 (1.1) 5.1 ± 2.2 (1.0)
rHIVI84V I84V 3.3 ± 0.3 (1.1) 313 ± 98 (13) 44 ± 18 (1.5) 6.4 ± 6.0 (1.3)
a

Data shown represent mean IC50 values (±1 standard deviation) derived from the results of three independent experiments conducted in triplicate. The IC50s were determined by employing MT-4 cells exposed to each infectious HIV-1 clone (50 TCID50s) in the presence of each inhibitor and using the inhibition of p24 Gag protein production as an end point. The fold change values in parentheses were calculated by dividing IC50s against each virus by the IC50 against rHIVWT. ND, not determined.

b

APV, amprenavir, a protease inhibitor.

c

AZT, zidovudine, a nucleoside reverse transcriptase inhibitor.

d

RAL, raltegravir, an integrase strand transfer inhibitor.