Table 3.
Recruitment of β‐arrestin‐2 induced by full‐length chemokines and peptides derived from their N‐terminal regions to CXCR4, CXCR3 and ACKR3
| Arrestin recruitment | |||||||
|---|---|---|---|---|---|---|---|
| Name | Sequence | CXCR4 | CXCR3 | ACKR3 | |||
| pEC50 ± SEM | Max (%) | pEC50 ± SEM | Max (%) | pEC50 ± SEM | Max (%) | ||
| CXCL12 | −8.03 ± 0.09 | 100 | <6.00 | 0 ± 1 | 8.81 ± 0.10 | 100 | |
| CXCL121–17 | KPVSLSYRCPCRFFESH | <4.00 | 18 ± 1 | <4.00 | 1 ± 1 | 6.11 ± 0.05 | 111 ± 9 |
| CXCL121–9 | KPVSLSYRS | <4.00 | 12 ± 2 | ND | 5.52 ± 0.09* | 97 ± 5 | |
| (CXCL121–9)2 | (KPVSLSYRC)2 | <4.00 | 25 ± 5 | ND | 6.50 ± 0.09* | 103 ± 4 | |
| CXCL121–17D | KPVSLSYRCPCRFFESH | <4.00 | 16 ± 4 | ND | 4.35 ± 0.43* | 72 ± 8 | |
| CXCL122–17 | ‐ PVSLSYRCPCRFFESH | <4.00 | 3 ± 1 | ND | 4.89 ± 0.22* | 100 ± 3 | |
| CXCL121–17/P2G | KGVSLSYRCPCRFFESH | <4.00 | 2 ± 7 | ND | 4.55 ± 0.47* | 63 ± 7 | |
| vCCL2 | <6.00 | 10 ± 1 | <6.00 | 0 ± 5 | 7.80 ± 0.09 | 71 ± 5 | |
| vCCL21–21 | LGASWHRPDKCCLGYQKRPLP | <4.00 | 18 ± 2 | <4.00 | 0 ± 2 | 6.31 ± 0.10 | 107 ± 8 |
| vCCL21–11 | LGASWHRPDKS | <4.00 | 0 ± 2 | ND | 5.31 ± 0.09* | 105 ± 6 | |
| (vCCL21–11)2 | (LGASWHRPDKC)2 | <4.00 | 0 ± 2 | ND | 5.48 ± 0.08ns | 107 ± 8 | |
| vCCL21–21D | LGASWHRPDKCCLGYQKRPLP | <4.00 | 0 ± 6 | ND | 4.27 ± 0.66* | 77 ± 7 | |
| CXCL11 | <6.00 | 8 ± 4 | 7.91 ± 0.16 | 100 | 8.47 ± 0.12 | 75 ± 3 | |
| CXCL111–17 | FPMFKRGRCLCIGPGVK | <4.52a | 13 ± 7 | <4.52a | 45 ± 8 | 6.22 ± 0.08a | 134 ± 6 |
| CXCL111–9 | FPMFKRGRS | ND | <4.00 | 35 ± 9 | 5.57 ± 0.12* | 102 ± 8 | |
| (CXCL111–9)2 | (FPMFKRGRC)2 | ND | 5.64 ± 0.08 | 89 ± 9 | 6.40 ± 0.07* | 132 ± 12 | |
| CXCL111–17D | FPMFKRGRCLCIGPGVK | ND | <4.52a | 28 ± 6 | 6.05 ± 0.10a ,ns | 136 ± 8 | |
| CXCL112–17 | ‐ PMFKRGRCLCIGPGVK | ND | <4.52a | 2 ± 3 | 5.81 ± 0.17a ,ns | 59 ± 15 | |
| CXCL111–17/P2G | FGMFKRGRCLCIGPGVK | ND | <4.52a | 5 ± 5 | 6.78 ± 0.09a , * | 126 ± 10 | |
| CXCL10 | ND | 7.59 ± 1.17 | 45 ± 6 | <6.00 | 21 ± 1 | ||
| CXCL101–17 | VPLSRTVRCTCISISNQ | ND | <4.00 | 0 ± 3 | <4.00 | 2 ± 2 | |
| CXCL9 | ND | 7.03 ± 0.21 | 46 ± 7 | ND | |||
| CXCL91–17 | TPVVRKGRCSCISTNQG | ND | <4.00 | 1 ± 2 | ND | ||
β‐arrestin‐2 recruitment was monitored in U87 cells using split Nanoluciferase complementation assay (n = 5). Peptides 1‐17 (for CXCL12 and CXCL11) and 1‐21 (for vCCL2) were considered as the standard, reference peptides and monomeric mutant peptides were compared with these. Where dimeric peptides were assessed, these were compared with their corresponding monomeric peptides.
*
P < 0.05, significantly different from standard peptides or from monomeric peptides.
a
Highest concentration tested 30 μM. ND: not determined. P < 0.05, significantly different from ; ns. not significant, P > 0.05.