Table 1 Kinetic parameters of NAD+ and its analogues for human PARP1
Substrate | kcat (min-1)a | Km (μM)a | kcat/Km (min−1 M-1) | |
|---|---|---|---|---|
PARP activity | NAD+ | 4.7 ± 0.4 | 145.4 ± 36.0 | 3.2 × 104 |
2 | 0.06 ± 0.01 | 218.1 ± 81.7 | 2.8 × 102 | |
6 | 4.1 ± 0.6 | 370.5 ± 104.8 | 1.1 × 104 | |
6-a-NAD+ | 1.9 ± 0.5 | 603.1 ± 307.9 | 3.2 × 103 | |
2-a-NAD+ | 1.4 ± 0.4 | 400.8 ± 238.2 | 3.5 × 103 | |
NADase activity | NAD+ | 0.39 ± 0.08 | 471.5 ± 187.4 | 8.3 × 102 |
2 | 0.02 ± 0.01 | 661.1 ± 489.0 | 0.3 × 102 | |
6 | 0.46 ± 0.17 | 326.9 ± 278.8 | 1.4 × 103 | |
6-a-NAD+ | 0.36 ± 0.02 | 370.8 ± 47.5 | 9.7 × 102 | |
2-a-NAD+ | 0.47 ± 0.13 | 545.9 ± 313.5 | 8.6 × 102 |
