Table 1. Pharmacological parameters obtained in β-arrestin-2 recruitment assays.
pEC50 (Emax) | CXCL12(WT) | CXCL12(R47E) | CXCL12(K56E) |
---|---|---|---|
CXCR4(WT) | 7.40 ± 0.04 (normalized to 100%) | 6.50 ± 0.10a (88.23% ± 6.6%) | 7.44 ± 0.06 (94.1% ± 2.9%) |
CXCR4(E26R) | 6.68 ± 0.07a (87.9% ± 3.8%b) | 6.88 ± 0.08c (101.8% ± 4.6%d) | ND |
CXCR4(D20R) | 6.79 ± 0.08a (78.54% ± 4.1%b) | 5.89 ± 0.24a (85.22% ± 22.9%be) | ND |
apEC50 significantly different from CXCR4(WT)-CXCL12(WT) according to the extra sum-of-squares F test (p < 0.05).
bEmax significantly different from CXCR4(WT)-CXCL12(WT) according to the extra sum-of-squares F test (p < 0.05).
cpEC50 significantly different from CXCR4(WT)-CXCL12(R47E) according to the extra sum-of-squares F test (p < 0.05).
dEmax significantly different from CXCR4(E26R)-CXCL12(WT) according to the extra sum-of-squares F test (p < 0.05).
eCurve incomplete and therefore Emax impossible to fit accurately.
Abbreviations: ND, not determined; pEC50, -log10 half maximal effective concentration; WT, wild type