Table 1.
Binding affinities of VEGF-A isoforms determined at VEGFR2.
| Isoform | Technique | Expression System | Binding Affinity * | Ref. |
|---|---|---|---|---|
| VEGF165a | Radioligand binding | Human kidney tissue in situ | 0.01–0.04 nM | [91] |
| HUVECs | 0.17 nM | [92] | ||
| Balb/c expressing VEGFR2 | 0.29 nM | [92] | ||
| COS-1 cells expressing VEGFR2 | 0.34 nM | [92] | ||
| PAE cells expressing VEGFR2 | 0.76 nM | [44] | ||
| PAE cells expressing VEGFR2 | 0.097 nM | [93] | ||
| SPR | VEGFR2 ligand binding domains (D2/D3) | 36.7 nM | [85] | |
| ITC | VEGFR2 ligand binding domains (D2/D3) | 18 nM | [85] | |
| VEGFR2 ligand binding domains (D2/D3) | 170 nM | [84] | ||
| VEGFR2 extracellular domain (D1–D7) | 2670 nM | [84] | ||
| NanoBRET | HEK293 cells expressing NanoLuc-VEGFR2 | 0.15 nM | [97] | |
| VEGF165b | NanoBRET | HEK293 cells expressing NanoLuc-VEGFR2 | 0.39 nM | [97] |
| VEGF121a | ITC | VEGFR2 extracellular domain (D1–D7) | 1120 nM | [84] |
| VEGFR2 ligand binding domains (D2/D3) | 93 nM | [84] | ||
| NanoBRET | HEK293 cells expressing NanoLuc-VEGFR2 | 0.34 nM | [97] | |
| VEGF145a | NanoBRET | HEK293 cells expressing NanoLuc-VEGFR2 | 1.82 nM | [97] |
| VEGF189a | NanoBRET | HEK293 cells expressing NanoLuc-VEGFR2 | 1.02 nM | [97] |
* Ligand binding affinity quantified as equilibrium dissociation constant of the “hot” ligand (Kd) or competing ligand (Ki). Abbreviations: Bioluminescence resonance energy transfer (BRET) using NanoLuciferase (NanoBRET); isothermal titration calorimetry (ITC); surface plasmon resonance (SPR).