Table 2.
Binding parameters of ligands on membranes expressing CXCR3 and/or CXCR4
| Radioligand | Displacer | CXCR3 | CXCR4 | CXCR3 + CXCR4 |
|---|---|---|---|---|
| [125I]-CXCL10 | CXCL10 | 9.6 ± 0.1 | ND | 9.6 ± 0.1 |
| CXCL12 | ND | ND | 8.9 ± 0.1 | |
| VUF10661 | 7.5 ± 0.1 | ND | 7.3 ± 0.1 | |
| VUF10085 | 7.1 ± 0.1 | ND | 7.2 ± 0.1 | |
| TAK-779 | 5.7 ± 0.1 | ND | 5.7 ± 0.1 | |
| AMD3100 | ND | ND | ND | |
| Bmax (fmol·μg–1) | 0.20 ± 0.02 | ND | 0.26 ± 0.04 | |
| [125I]-CXCL12 | CXCL10 | ND | ND | 8.8 ± 0.2 |
| CXCL12 | ND | 9.5 ± 0.1 | 9.5 ± 0.2 | |
| VUF10661 | ND | ND | 6.9 ± 0.3 | |
| VUF10085 | ND | ND | ND | |
| TAK-779 | ND | ND | ND | |
| AMD3100 | ND | 6.8 ± 0.2 | 7.3 ± 0.1 | |
| Bmax (fmol·μg–1) | ND | 1.58 ± 0.15 | 1.08 ± 0.14 |
Binding parameters of the CXCR3 ligands CXCL10 (chemokine), VUF10661 (small agonist), TAK-779 and VUF10085 (antagonists) and the CXCR4 ligands CXCR4L12 (chemokine) and AMD3100 (antagonist) for their cognate receptors were determined in the absence and presence of CXCR4 and CXCR3, respectively. pIC50 values were determined using displacement of [125I]-CXCL10 and [125I]-CXCL12 from membrane preparations of HEK293T cells transfected with CXCR3, CXCR4 or both receptors. pIC50 values are given as averages ± SEM of two or more independent experiments performed in triplicate.
ND: value could not be determined.