Table 2.
Inhibition data for TcdB-GTD and TcdA-GTD glucohydrolase and glucosyltransferase activity.
| Inhibitor | Ki TcdB-GTD glucohydrolase activity (µM) | Ki TcdB-GTD glucosyltransferase activity (µM) | Ki TcdA-GTD glucosyltransferase activity (µM) |
|---|---|---|---|
| Gluconolactone | 413.6 ± 45.5 | 439.7 ± 34.4 | – |
| Deoxynojirimycin | NI | NI | – |
| Isofagomine | 4.8 ± 0.2 | 1.4 ± 0.1 | 0.24 ± 0.01 |
| Noeuromycin | 12.0 ± 1.6 | 10.6 ± 1.0 | 4.7 ± 0.2 |
| Australine HCl | NI | 1570 ± 430 | – |
| Castanospermine | 3400 ± 200 | 680 ± 20 | – |
| Swainsonine | NI | NI | – |
| UDP | – | 11.5 ± 2.9 | 81.1 ± 3.1 |
| Isofagomine (2 x Ki UDP) | – | 0.29 ± 0.06 | 0.016 ± 0.002 |
| Noeuromycin (2 x Ki UDP) | – | 4.4 ± 0.1 | 0.214 ± 0.055 |
Inhibition constants (Ki) for transition state analogues tested for inhibition of GH and GT activity of TcdB-GTD and TcdA-GTD.
NI: No inhibition (Ki > 10 mM)
The data represents the mean value of 3 independent assays ± SEM
Source data are provided as a Source Data file.