TABLE 3.
IC50s of L-731,988 and l-CA against reference and mutant IN proteins
| IN protein | IC50 (μM)a
|
|||
|---|---|---|---|---|
|
l-CA
|
L-731,988 (ST, U5V1P) | |||
| Disintegration, dBY-1 | 3′-EP, V1-V2 | ST, U5V1P | ||
| Reference | 0.100 (0.03)1 | 0.13 (0.006) | 0.077 (0.02) | 0.48 (0.30) |
| G149S | 0.402 (0.20) | 0.40 (0.09) | 0.55 (0.19) | 5.2 (0.66) |
| K156A | 2.39 (0.46) | 3.6 (1.26) | 0.93 (0.36) | 1.5 (0.49) |
| K156R | 0.074 (0.02) | 2.3 (0.74) | 2.36 (0.48) | 0.20 (0.005) |
| C65S-K156N | 2.89 (1.14) | 0.64 (0.30) | 1.13 (0.25) | 5.0 (0.66) |
| E92K | 2.25 (0.90) | >>25 | 1.02 (0.30) | 0.25 (0.01) |
| Q148A | 0.95 (0.32) | 6.6 (4.65) | 1.60 (0.45) | 10.8 (5.0) |
| H67D-G140A | 1.79 (0.23) | 6.0 (1.23) | ND | ND |
a
Values in parentheses are 1 standard deviation. 3′-EP, 3′-end processing; ST, strand transfer; ND, not determined since no strand transfer products were observed.