Table 1.
INI off-rate from IN-DNA complexes at 37°C
IN |
koffa (s−1) (×10−6) |
Relative koff vs wild type |
||||
---|---|---|---|---|---|---|
DTG | RAL | ELV | DTG | RAL | ELV | |
Wild type | 2.7 ± 0.4 | 22 ± 2 | 71 ± 4 | 1.0 | 1.0 | 1.0 |
E92Q | 11.4 ± 0.3 | 59 ± 9 | 430 ± 20 | 4.2 | 2.7 | 6.1 |
E138K | 2.3 ± 0.2 | 17 ± 0.3 | 52 ± 1 | 0.9 | 0.8 | 0.7 |
G140S | 9.6 ± 0.8 | 44 ± 3 | 180 ± 20 | 3.6 | 2.0 | 2.5 |
Y143C | 3.2 ± 0.1 | 96 ± 4 | 91 ± 2 | 1.2 | 4.4 | 1.3 |
Y143H | 4.4 ± 0.2 | 78 ± 2 | 120 ± 6 | 1.6 | 3.5 | 1.7 |
Y143R | 4.6 ± 0.3 | 176 ± 4 | 116 ± 5 | 1.7 | 8.0 | 1.6 |
Q148H | 37 ± 3 | 1,160 ± 120 | 1,130 ± 140 | 13.7 | 53 | 16 |
Q148K | 18 ± 5 | 730 ± 130 | NDb | 6.7 | 33 | |
Q148R | 21 ± 2 | 480 ± 80 | ND | 7.8 | 22 | |
N155H | 20 ± 2 | 300 ± 80 | 500 ± 140 | 7.4 | 14 | 7.0 |
E92Q/N155H | 49 ± 3 | 770 ± 70 | ND | 18 | 35 | |
E138K/Q148R | 53 ± 10 | 900 ± 340 | ND | 20 | 41 | |
G140S/Q148H | 58 ± 8 | 1,130 ± 210 | ND | 22 | 51 |
koff values represent means and standard deviations for 3 to 8 independent experiments.
ND, not determined due to low signal with [3H]ELV.