Table 2 Inhibition data for TcdB-GTD and TcdA-GTD glucohydrolase and glucosyltransferase activity.

From: Inhibition of Clostridium difficile TcdA and TcdB toxins with transition state analogues

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

  1. Inhibition constants (Ki) for transition state analogues tested for inhibition of GH and GT activity of TcdB-GTD and TcdA-GTD.
  2. NI: No inhibition (Ki > 10 mM)
  3. The data represents the mean value of 3 independent assays ± SEM
  4. Source data are provided as a Source Data file.
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