Characterization of hCXCR4 mutants by 125I-SDF-1α binding and SDF-1 α-induced calcium flux signaling in transfected Cf2Th cells
125I-SDF-1α Binding Kd | Mean Relative Bmaxa ± S.D. | SDF-1α Calcium Flux Signaling EC50 | Wild-Type Response in Presence of 200 nM SDF-1α | |
|---|---|---|---|---|
| nM | % | nM | % | |
| WT | 35.8 | 100 | 34.0 | 100 |
| Y45A | 22.8 | 70.8 ± 3.7 | 33.9 | 25.6 |
| W94A | 54.9 | 43.4 ± 2.8 | 45 | 19.8 |
| D97N | 47.6 | 72.6 ± 24.8 | N.R. | N.R. |
| Y116A | 33.7 | 170.7 ± 7.9 | N.R. | N.R. |
| Y121A | 86.2 | 58.4 | 100 | 64.9 |
| D171N | 73.6 | 39.7 ± 1.1 | 137.9 | 60.1 |
| N176A | 15.1 | 80.8 ± 26.7 | 59.4 | 68.0 |
| R183A | 16.4 | 79.2 ± 20.7 | 42.9 | 71.6 |
| V196A | 22.7 | 89.2 ± 8.7 | 138.2 | 105.6 |
| H203A | 42.3 | 97.9 ± 22.9 | 26.1 | 103.8 |
| Y255A | 11.8 | 96.7 ± 3.3 | 42.0 | 41.3 |
| D262N | 80.3 | 32.5 ± 2.1 | 96.5 | 60.0 |
| H281A | 6.9 | 133.2 ± 10.0 | 136.3 | 18.5 |
| E288A | 44.1 | 53.1 | N.R. | N.R. |
N.R., no response.
↵ a The relative percentage Bmax = Bmax in cpm of the mutant/wild type in the same experiment.