Table 1

Binding constants of selected CXC-chemokines for the HHV8-encoded ORF74 receptor using different radiolabeled ligands. The ORF-74 receptor was transiently transfected in COS-7 cells and competition binding experiments were performed as described under Experimental Procedures. IC50 values were determined either in competition against 125I-GROα (B max = 44 ± 10 fmol/105 cell), 125I-IL8 (B max = 42 ± 12 fmol/105 cell), or125I-IP-10 (B max = 28 ± 5 fmol/105 cell). Shown are mean ± S.E. of the indicated number of experiments (n). The “fold difference” measured in affinity when using 125I-GROα or125I-IP-10 versus 125I-IL8 as radioactive ligand is listed in a separate column.

AgonistsNeutral LigandsInverse Agonists
LigandIC50Hill slopeFoldLigandIC50Hill slopeFoldLigandIC50Hill slopeFold
nM (n) nM (n) nM (n)
125I-GROαGROα0.10  ± 0.02 (11)−1.27  ± 0.090.4IL-81332  ± 795 (5)−0.94  ± 0.25888IP-102.3  ± 0.60 (3)−0.77  ± 0.060.55
GROβ0.22  ± 0.05 (5)−0.79  ± 0.110.7NAP-282  ± 12 (5)−0.91  ± 0.0823GCP-20.44  ± 0.01 (3)−0.94  ± 0.120.73
GROγ0.06  ± 0.01 (5)−0.90  ± 0.060.2ENA-78173  ± 31 (3)−1.20  ± 0.0916SDF-1α13  ± 1.4 (4)−0.87  ± 0.102
125I-IL-8GROα0.23  ± 0.07 (5)−1.04  ± 0.091IL-81.5  ± 0.36 (5)−0.91  ± 0.081IP-104.2  ± 1.1 (3)−1.31  ± 0.091
GROβ0.34  ± 0.10 (5)−1.05  ± 0.101NAP-23.6  ± 0.59 (4)−0.92  ± 0.101GCP-20.60  ± 0.08 (3)−1.19  ± 0.061
GROγ0.37  ± 0.09 (5)−1.49  ± 0.141ENA-7811  ± 2.9 (2)−0.82  ± 0.021SDF-1α6.7  ± 1.6 (5)−1.11  ± 0.141
125I-IP10GROα0.83  ± 0.03 (5)−0.95  ± 0.143.6IL-81627  ± 712 (3)−0.41  ± 0.191085IP-100.62  ± 0.21 (7)−0.99  ± 0.040.14
GROβ1.60  ± 0.18 (3)−1.00  ± 0.074.4NAP-2839  ± 56 (3)−0.58  ± 0.10233GCP-21.3  ± 0.38 (3)−1.00  ± 0.132.2
GROγ0.82  ± 0.16 (3)−1.35  ± 0.222.2ENA-78515  ± 251 (3)−1.30  ± 0.1447SDF-1α17  ± 9 (3)−0.99  ± 0.382.5