Table 5. Kinetic parameters of VEGF and anti-VEGF.
Measured parameters | Tissue parameters | ||||
VEGF binding to VEGFR-1 | Value | Unit | Value (Tissue) | Value (Blood) | Unit |
kon | 3.00×107 | M−1s−1 | 2.65×10−1 | 6.15×10−2 | (pmol/cm3 tissue)−1s−1 |
koff | 1.00×10−3 | s−1 | |||
Kd | 33 | pM | 3.73×10−3 | 1.61×10−2 | pmol/cm3 tissue |
VEGF binding to VEGFR-2 | |||||
kon | 1.00×107 | M−1s−1 | 8.84×10−2 | 2.05×10−2 | (pmol/cm3 tissue)−1s−1 |
koff | 1.00×10−3 | s−1 | |||
Kd | 1.00×102 | pM | 1.13×10−2 | 4.88×10−2 | pmol/cm3 tissue |
VEGF164 binding to NRP-1 | |||||
kon | 3.13×106 | M−1s−1 | 2.77×10−2 | 6.41×10−3 | (pmol/cm3 tissue)−1s−1 |
koff | 1.00×10−3 | s−1 | |||
Kd | 3.12×102 | pM | 3.52×10−2 | 1.52×10−1 | pmol/cm3 tissue |
VEGF164 binding to GAGs | |||||
kon | 4.20×105 | M−1s−1 | 3.72×10−3 | - | (pmol/cm3 tissue)−1s−1 |
koff | 1.00×10−2 | s−1 | |||
Kd | 2.40×101 | nM | 2.71 | - | pmol/cm3 tissue |
Coupling of NRP-1 and VEGFR-2 | |||||
kc V164R2,N1 | 3.10×1013 | (mol/cm2)−1s−1 | 1.99×10−1 | 1.59×10−2 | (pmol/cm3 tissue)−1s−1 |
koff V164R2,N1 | 1.00×10−3 | s−1 | |||
kc V164N1,R2 | 1.00×1014 | (mol/cm2)−1s−1 | 6.41×10−1 | 5.13×10−2 | (pmol/cm3 tissue)−1s−1 |
koff V164N1,R2 | 1.00×10−3 | s−1 | |||
Coupling of NRP-1 and VEGFR-1 | |||||
kc R1,N1 | 1.00×1014 | (mol/cm2)−1s−1 | 6.41×10−1 | 5.13×10−2 | (pmol/cm3 tissue)−1s−1 |
kdissoc R1,N1 | 1.00×10−2 | s−1 | |||
VEGFR internalization | |||||
kint, R | 2.80×10−4 | s−1 | |||
kint, C | 2.80×10−4 | s−1 | |||
VEGF binding to anti-VEGF * | |||||
kon | 1.13×108 | M−1s−1 | 1.00 | 2.32×10−1 | (pmol/cm3 tissue)−1s−1 |
koff | 4.23×10−5 | s−1 | |||
Kd | 0.37 | pM | 4.18×10−5 | 1.81×10−4 | pmol/cm3 tissue |
*Optimized parameter values.
Conversions:
Tissue: 1.13×108 (pmol/cm3 tissue)/M and 1.56×1014 (pmol/cm3 tissue)/(mol/cm2 EC).
Blood: 4.88×108 (pmol/cm3 tissue)/M and 1.95×1015 (pmol/cm3 tissue)/(mol/cm2 EC).