Table 1.
Kinetic parameters and biological effects of trx-AF17121 and its mutational variants
|
kon × 10-4 (M-1 s-1) |
koff × 103 (s-1) |
Kd × 108 (M) |
Chi2 | # IC50 | |
|---|---|---|---|---|---|
| AF17121 | 13 ± 1 | 2.9 ± 0.2 | 2.3 ± 0.2 | 0.11 ± 0.03 | 1 |
| D2A-E3A | 1.8 ± 0.4 | 5.6 ± 0.5 | 31 ± 3 | 0.10 ± 0.02 | 4 |
| R6A | N.D. | N.D. | |||
| R6K | N.D. | N.D.1 | |||
| H11A | 7.7 ± 0.2 | 17 ± 1 | 22 ± 2 | 0.33 ± 0.05 | 8.7 1 |
| E17A-E18A | 5.9 ± 0.2 | 10 ± 1 | 17 ± 1 | 0.50 ± 0.15 | 1.8 |
| non-acid | 0.76 ± 0.04 | 12 ± 1 | 160 ± 12 | 0.89 ± 0.36 | N.D.1 |
N.D., not detected.
#
The relative IC50 values are the concentrations to inhibit half-maximal proliferation of TF-1 cell. Data are taken from R. Piotr et al. (2004).
1
Unpublished data (M. Bhattacharya et al).