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Table 2 Binding constants (KD) of t-PA-peptide-1 and its derivates with galectins Gal-1, Gal-3 and Gal-4

From: Synthesis and functionalization of protease-activated nanoparticles with tissue plasminogen activator peptides as targeting moiety and diagnostic tool for pancreatic cancer

T-PA peptide

Label

Modification

Galectin

KD [µM]

Fold diff.

rh t-PA protein

N-Fluo.

None = (Asn16)

Gal-1

4.92

1

Peptide-1(pep-1)

N-Fluo.

None

Gal-1

141.1

−28.7

t-PA-pep-1

C-Fluo.

None

Gal-1

  

t-PA-pep-1gal

C-TAMRA

Ser16-α d-galactose

Gal-1

0.66

7.5

t-PA-pep-1lac

N-Fluo.

Ser16-β d-lactose

Gal-1

0.286

17

t-PA-pep-1lac

C-Fluo.

Ser16-β d-lactose

Gal-1

0.20

25

rh t-PA protein

N-Fluo.

None = (Asn16)

Gal-3

7.68

1

t-PA-pep-1

N-Fluo.

None

Gal-3

272.0

−35.4

t-PA-pep-1gal

C-TAMRA

Ser16b-α d-galactose

Gal-3

39.1

−5.1

t-PA-pep-1lac

C-Fluo.

Ser16b-β d-lactose

Gal-3

0.73

10.4

rh t-PA protein

N-Fluo.

none = (Asn16)

Gal-4

51.2

1

t-PA-pep-1

N-Fluo.

none

Gal-4

34.0

1.5

t-PA-pep-1gal

C-TAMRA

Ser16-β d-galactose

Gal-4

211

−4.2

t-PA-pep-1lac

C-Fluo.

Ser16-β d-lactose

Gal-4

12.7

4.03

  1. The MST was performed with the tPA peptide and its variants (N- or C-terminal fluorescence-labeled and glycosylated forms) in the presence of human galectins
  2. Italic values indicate significance of p < 0.01