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. 2018 Mar 23;175(9):1419–1438. doi: 10.1111/bph.14132

Table 4.

Binding and signalling properties of CXCL11 variants towards CXCR3 and ACKR3

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.