Table 4.
Name | Sequence | Binding competition | cAMP | Calcium | Arrestin recruitment | ||||||
---|---|---|---|---|---|---|---|---|---|---|---|
CXCR3 | ACKR3 | CXCR3 | CXCR3 | CXCR3 | ACKR3 | ||||||
pIC50 ± SEM | pIC50 ± SEM | pEC50 ± SEM | Max (%) | pEC50 ± SEM | Max (%) | pEC50 ± SEM | Max (%) | pEC50 ± SEM | Max (%) | ||
CXCL11 WT | 1‐FPMFKRGRCLCIGPGVKAVK‐73 | 8.48 ± 0.09 | 6.52 ± 0.05 | 8.21 ± 0.11 | 100 | 7.80 ± 0.07 | 100 | 7.57 ± 0.07 | 100 | 7.46 ± 0.09 | 100 |
CXCL11Nloop10 | 1‐FPMFKRGRCLCISISNQAVK‐73 | 7.41 ± 0.11* | 6.11 ± 0.07* | 7.93 ± 0.13 ns | 81 | 7.98 ± 0.11ns | 92 | 7.42 ± 0.08ns | 89 | 7.68 ± 0.10 ns | 85 |
CXCL11Nloop12 | 1‐FPMFKRGRCLCRFFESHAVK‐73 | 6.91 ± 0.08* | 6.29 ± 0.04* | 6.85 ± 0.14* | 102 | 7.02 ± 0.06* | 79 | <6.00 | 41 | 7.32 ± 0.09ns | 84 |
CXCL113–73 | 3‐MFKRGRCLCIGPGVKAVK‐73 | 6.90 ± 0.09* | 5.78 ± 0.07* | 8.39 ± 0.21ns | 54 | <6.00 | 37 | <6.00 | 22 | 7.15 ± 0.08* | 81 |
CXCL115–73 | 5‐KRGRCLCIGPGVKAVK‐73 | 6.18 ± 0.05* | 5.29 ± 0.01* | <6.00 | <6.00 | <6.00 | 16 | <6.00 | 30 | ||
CXCL117–73 | 7‐RCLCIGPGVKAVK‐73 | <5.00 | <5.00 | <6.00 | <6.00 | <6.00 | 15 | <6.00 | 22 | ||
CXCL11P2G | 1‐FGMFKRGRCLCIGPGVKAVK‐73 | 9.63 ± 0.09* | 8.76 ± 0.05* | 7.86 ± 0.15ns | 100 | 7.40 ± 0.04* | 83 | 7.22 ± 0.14ns | 61 | 7.99 ± 0.07* | 136 |
Binding competition studies with radiolabeled CXCL11 (CXCR3) or CXCL12 (ACKR3) were performed in HEK293T cells (n = 5). β‐arrestin‐2 recruitment was monitored by BRET in HEK293T cells expressing YFP‐fused receptors and Rluc‐fused β‐arrestin‐2.
P < 0.05, significantly different from WT peptide; ns. not significant.