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Table 2 Inhibition constants calculated for the inhibition of wild-type and variant ppFhCL3 against recombinant F. hepatica and human cathepsin peptidases

From: Regulation of the Fasciola hepatica newly excysted juvenile cathepsin L3 (FhCL3) by its propeptide: a proposed ‘clamp-like’ mechanism of binding and inhibition

Cathepsin

Inhibition Ki (nM)

ppFhCL3

ppFhCL3

Tyr46Lys47/Ala46Ala47

ppFhCL3

Leu66/Gly66

ppFhCL3

Glu68/Arg68

FhCL1

0.04

(±0.006)

1.26

(±0.2)

0.05

(±0.004)

0.3

(±0.001)

FhCL2

0.004

(±0.002)

> 10.000*

> 10,000

0.02

(±0.01)

FhCL3

< 0.002*

> 10.000

8.00

(±2.3)

0.002

(±0.001)

HsCL

26.6

(±0.4)

> 10.000

> 10.000

6.04

(±0.44)

HsCK

2.0

(±0.5)

> 10.000

> 10.000

1.40

(±0.2)

  1. * Ki values > 10,000 nM and < 0.002 could not be calculated accurately