| Author |
Das (2004) | | Title |
Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian | | Citation |
J Med Chem |
| | | SelectedGene |
RT | | SelectedType |
Lab | | NumIsolates |
15 |
|
|
Lab RT Isolates (including Susceptibility Data) | |
| Isolate | NRTIDRMs | NNRTIDRMs | Other Mutations | Method | Drug | Result | Fold Res. |
|---|
| 100I | | L100I | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | 220.0 |
| | | | | Pauwels | EFV | | 38.0 |
| | | | | Pauwels | ETR | | 3.0 |
| | | | | Pauwels | NVP | | 7.5 |
| 100I+103N | | L100I, K103N | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | >600.0 |
| | | | | Pauwels | EFV | | >1000.0 |
| | | | | Pauwels | ETR | | 19.0 |
| | | | | Pauwels | NVP | | >100.0 |
| 101E | | K101E | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | 12.0 |
| | | | | Pauwels | EFV | | 6.0 |
| | | | | Pauwels | ETR | | 6.0 |
| | | | | Pauwels | NVP | | 51.0 |
| 101E+103N | | K101E, K103N | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | 94.0 |
| | | | | Pauwels | EFV | | 180.0 |
| | | | | Pauwels | ETR | | 3.0 |
| | | | | Pauwels | NVP | | >100.0 |
| 103N | | K103N | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | 106.0 |
| | | | | Pauwels | EFV | | 39.0 |
| | | | | Pauwels | ETR | | 1.0 |
| | | | | Pauwels | NVP | | 29.0 |
| 103N+181C | | K103N, Y181C | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | >600.0 |
| | | | | Pauwels | EFV | | 43.0 |
| | | | | Pauwels | ETR | | 4.0 |
| | | | | Pauwels | NVP | | >100.0 |
| 106A | | V106A | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | 140.0 |
| | | | | Pauwels | ETR | | 2.0 |
| | | | | Pauwels | NVP | | 28.0 |
| 106A+227L | | V106A, F227L | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | 10.0 |
| | | | | Pauwels | EFV | | 39.0 |
| | | | | Pauwels | ETR | | 4.0 |
| | | | | Pauwels | NVP | | >100.0 |
| 138K | | E138K | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | 3.5 |
| | | | | Pauwels | EFV | | 2.0 |
| | | | | Pauwels | ETR | | 5.0 |
| | | | | Pauwels | NVP | | 5.7 |
| 179E | | V179E | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | 47.0 |
| | | | | Pauwels | EFV | | 6.0 |
| | | | | Pauwels | ETR | | 3.0 |
| | | | | Pauwels | NVP | | 21.0 |
| 181C | | Y181C | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | 84.0 |
| | | | | Pauwels | EFV | | 2.0 |
| | | | | Pauwels | ETR | | 7.0 |
| | | | | Pauwels | NVP | | 63.0 |
| 188L | | Y188L | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | 12.0 |
| | | | | Pauwels | EFV | | 140.0 |
| | | | | Pauwels | ETR | | 5.0 |
| | | | | Pauwels | NVP | | 79.0 |
| 190A | | G190A | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | 1.0 |
| | | | | Pauwels | EFV | | 11.0 |
| | | | | Pauwels | ETR | | 1.0 |
| | | | | Pauwels | NVP | | 41.0 |
| 190S | | G190S | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | 1.0 |
| | | | | Pauwels | EFV | | 340.0 |
| | | | | Pauwels | ETR | | 2.0 |
| | | | | Pauwels | NVP | | >100.0 |
| 227C | | F227C | K122E, F214L, A272P, K277R, M357T, A376T, A400T, N447S, D460N, S468T, S519N | Pauwels | DLV | | 75.0 |
| | | | | Pauwels | EFV | | 180.0 |
| | | | | Pauwels | ETR | | 27.0 |
| | | | | Pauwels | NVP | | >100.0 |