Table 7.
Resistance profiles of inhibitors 36 and 37
| Virusa | IC50 values, nM (fold change) | |||
|---|---|---|---|---|
|
|
||||
| 36 | 37 | DRV | APV | |
| HIV-1ERS104pre (WT) | 20 | 6 | 3.5 | 33 |
| HIV-1TM (MDR) | 220 (11) | 64 (10) | 4 (1) | 290 (9) |
| HIV-1MM (MDR) | 250 (13) | 110 (18) | 17 (5) | 300 (9) |
| HIV-1JSL (MDR) | 500 (25) | 330 (55) | 26 (7) | 430 (13) |
| HIV-1B (MDR) | 340 (17) | 230 (38) | 26 (7) | 320 (10) |
| HIV-1C (MDR) | 210 (11) | 160 (27) | 7 (2) | 230 (7) |
| HIV-1G (MDR) | 360 (18) | 300 (50) | 7 (2) | 340 (10) |
| HIV-1A (MDR) | 20 (1) | 13 (2) | 3 (1) | 100 (3) |
a
Amino acid substitutions in the protease-encoding region compared to type B: L63P in HIV-1ERS104pre; L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, I93L in HIV-1TM; L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, Q92K in HIV-1MM; L10I, L24I, L33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, V82A in HIV-1JSL; L10I, K14R, L33I, M36I, M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L in HIV-1B; L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q,V82A, and L89M in HIV-1C; L10I, V11I, T12E, I15V, L19I, R41K, M46L, L63P, A71T, V82A, and L90M in HIV-1G; L10I, I15V, E35D, N37E, K45R, I54V, L63P, A71V, V82T, L90M, I93L, C95F in HIV-1A