Chemical features and VEGF binding activity of K5 derivatives
GAG | SO3−/COO− ratio | Average molecular weight (Da) | VEGF-mediated cell-cell adhesion ID50 (µg/mL) | SPR | |
---|---|---|---|---|---|
VEGF/heparin binding ID50 (µg/mL) | VEGF/sVEGFR2 binding ID50 (µg/mL) | ||||
K5 | 0 | 30,000 | No inhibition | No inhibition | No inhibition |
K5-NS | 1.00 | 15,000 | >100 | 4.5 | 12.0 |
K5-N,OS(L) | 1.70 | 13,000 | 10.2 | 5.0 | 9.5 |
K5-N,OS(H) | 3.77 | 15,000 | 0.5 | 0.005 | 0.2 |
Heparin | 2.14 | 13,600 | 0.2 | 0.4 | 1.0 |
Sulfate/carboxyl ratio (SO3−/COO−) and molecular weight values are from Leali et al. (28). GAGs were assessed for the capacity to inhibit the formation of HSPG/VEGF/VEGFR2 ternary complexes in a VEGF-mediated cell-cell adhesion assay and to prevent the binding of VEGF to heparin and sVEGFR2 immobilized to Biacore sensor chips.