Table 1.

Interactions between purified human uPAR and various peptide antagonists as assessed by surface plasmon resonance

Peptide antagonistkon (105 mol/L−1 s−1)koff (10−4 s−1)KD (nmol/L)IC50 (nmol/L)
DOTA-AE105mutNDNDND0.3 × 106
  • NOTE: Purified, recombinant human uPAR (residues 1-283) was immobilized on a Biacore CM5-sensor chip and the interaction with 2-fold serial dilution series of the synthetic peptides in running buffer was measured at 20°C and a flow rate of 50 μL/min. Kinetic rate constants were derived by curve fitting to the recorded sensorgrams using nonlinear regression analysis and KD values were calculated as koff/kon (18). IC50 values were derived by solution competition assays using Biacore as described in Materials and Methods.