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Table 2 Kinetic parameters for the hydrolysis of the FRET peptides derived from sequences that span the cleavage sites for activation of protease-activated receptor (PAR) 1,3 and 4 by human cathepsins, L, S, V and B

From: Cathepsin K induces platelet dysfunction and affects cell signaling in breast cancer - molecularly distinct behavior of cathepsin K in breast cancer

Enzyme

 

Peptide

Abz-eptidyl-EDDap

%

kcat (s-1)

Km (µM)

Kcat/Km (s-1 µM-1)

Cathepsin L

 

Z-FR-MCA[27]

-

-

17.6

1.3

13.5

-

PAR 1

TL↓DPRSFL↓L↓Q↓

L↓D-30/L↓L-32/L↓Q-16/Q↓Eddnp-22

3.5

2.2

1.6

+

PAR 3

TLPIK↓TFR↓GQ

K↓T-45/R↓G-55

10.6

3.9

2.7

nh

PAR 4

LPAPRGYPGQ

-

-

-

-

Cathepsin S

 

Z-FR-MCA[32]

-

-

2

21

0.09`

+

PAR 1

TLDPR↓SFLL↓Q

R↓S-24/L↓Q-76

1.2

4.2

0.29

+

PAR 3

TLPIK↓TFR↓GQ

K↓T-36/R↓G-64

0.3

8.1

0.04

-

PAR 4

LPAPRG↓YPGQ

-

   

Cathepsin V

 

Z-FR-MCA [27]

-

-

0.71

6.4

0.11

-

PAR 1

TLDPR↓SFL↓L↓Q

R↓S-55/L↓L-2/L↓Q-R3

0.01

1.0

0.01

+

PAR 3

TLPIK↓TF↓R↓GQ

K↓T-74/F↓R-15/R↓G-11

0.78

1.9

0.41

+

PAR 4

LPAPR↓GYPG↓Q

R↓G-75/G↓Q-43

-

-

-

Cathepsin B

 

Abz-FRA (eDnp)K[34]

-

-

16.9

13.4

1.33

nh

PAR 1

TLDPRSFLLQ

-

-

-

-

nh

PAR 3

TLPIKTFRGQ

-

-

-

-

nh

PAR 4

LPAPRGYPGQ

-

-

-

-

  1. Assay conditions: [32] Bromme et al., 1994; [27] = Bromme et al., 1999; [34] Almeida et al., 2001. Enrichment of PAR-2 of kinetic parameters see Supplementary content, Table S1