TABLE 1.
Inhibition of GpppA formation with GDP analogues
| GDP analogue (abbreviation) | IC50 (μM)a | Estimated Ki (μM)b |
|---|---|---|
| ADP | 23 ± 2 | 2.6 |
| IDP | 6.4 ± 0.2 | 0.70 |
| XDP | 58 ± 3 | 6.4 |
| 2-Aminopurine-riboside 5′-diphosphate (APDP) | 1.3 ± 0.1 | 0.14 |
| 2,6-Diaminopurine-riboside 5′-diphosphate (DAPDP) | 0.37 ± 0.02 | 0.036 |
| 7-Deazaguanosine 5′-diphosphate (7-deaza-GDP) | 0.40 ± 0.04 | 0.040 |
| 7-Methylguanosine 5′-diphosphate (m7GDP) | 0.39 ± 0.02 | 0.038 |
| 1-Methylguanosine 5′-diphosphate (m1GDP) | 1.6 ± 0.2 | 0.17 |
| 2′-Deoxyguanosine 5′-diphosphate (2′-dGDP) | 0.53 ± 0.01 | 0.053 |
| 3′-Deoxyguanosine 5′-diphosphate (3′-dGDP) | 0.57 ± 0.03 | 0.058 |
| 2′,3′-Dideoxyguanosine 5′-diphosphate (ddGDP) | 3.5 ± 0.3 | 0.38 |
| Ribavirin 5′-diphosphate (RDP) | 8.6 ± 0.4 | 0.95 |
a
Oligo-RNA capping was performed with 0.25 μM μM [α-32P]GDP and 2.5 μM pppAACAG in the presence or absence of various concentrations of GDP analogues. Absolute IC50s were determined as described in Materials and Methods. Data represent the means and standard deviations from three independent experiments.
b
IC50s were converted to Ki values against GDP as described in Materials and Methods.