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

Table 1.

Binding properties of full‐length chemokines and peptides derived from their N‐terminal regions towards CXCR4 and ACKR3

Name Sequence Binding competition
CXCR4 ACKR3
pIC50 ± SEM pIC50 ± SEM
CXCL12 7.89 ± 0.04 8.74 ± 0.07
CXCL121–17 KPVSLSYRCPCRFFESH ~4.00 5.39 ± 0.10
CXCL121–9 KPVSLSYRS <3.00 5.05 ± 0.13ns
(CXCL121–9)2 (KPVSLSYRC)2 5.31 ± 0.16 5.65 ± 0.09*
CXCL121–17D KPVSLSYRCPCRFFESH ~4.00 <4.00
CXCL122–17 PVSLSYRCPCRFFESH ~4.00 5.23 ± 0.25ns
CXCL121–17/P2G KGVSLSYRCPCRFFESH <4.00 4.22 ± 1.19ns
vCCL2 7.70 ± 0.06 7.47 ± 0.07
vCCL21–21 LGASWHRPDKCCLGYQKRPLP 5.71 ± 0.24 5.77 ± 0.13
vCCL21–11 LGASWHRPDKS ~4.00 5.27 ± 0.24ns
(vCCL21–11)2 (LGASWHRPDKC)2 6.67 ± 0.06 5.59 ± 0.13ns
vCCL21–21 D LGASWHRPDKCCLGYQKRPLP 6.21 ± 0.21ns ~4.00
CXCL11 <6.00 8.45 ± 0.03
CXCL111–17 FPMFKRGRCLCIGPGVK <4.52a 5.46 ± 0.12a
CXCL111–9 FPMFKRGRS ND 5.09 ± 0.13ns
(CXCL111–9)2 (FPMFKRGRC)2 ND 6.03 ± 0.14*
CXCL111–17D FPMFKRGRCLCIGPGVK ND 5.06 ± 0.12*, a
CXCL112–17 PMFKRGRCLCIGPGVK ND <4.52a
CXCL111–17/P2G FGMFKRGRCLCIGPGVK ND 6.72 ± 0.09*, a
CXCL10 <6.00 <6.00
CXCL101–17 VPLSRTVRCTCISISNQ <4.52a <4.52*, a

Binding competition studies with fluorescently labelled CXCL12 were performed in U87 cells (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; ns, not significant, P > 0.05.

a

Highest concentration tested 30 μM. ND: not determined.

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