Nomenclature |
CXCR1
|
CXCR2
|
CXCR3
|
HGNC, UniProt |
CXCR1, P25024
|
CXCR2, P25025
|
CXCR3, P49682
|
Endogenous
agonists |
CXCL8 (CXCL8, P10145)
(pK
i 8.8–9.5) [142, 675, 1068, 2032, 2049], CXCL6 (CXCL6, P80162)
(pK
i 7) [2053] |
CXCL1 (CXCL1, P09341)
(Selective) (pK
i 8.4–9.7) [675, 1068, 2049], CXCL8 (CXCL8, P10145)
(pK
i 8.8–9.5) [142, 675, 1068, 2032, 2049], CXCL7 (PPBP, P02775)
(Selective) (pIC50 6.3–9.3) [16], CXCL3 (CXCL3, P19876)
(Selective) (pIC50 7.8–9.2) [16], CXCL2 (CXCL2, P19875)
(Selective) (pIC50 7–9.1) [16], CXCL5 (CXCL5, P42830)
(Selective) (pIC50 6.9–9) [16], CXCL6 (CXCL6, P80162)
(pK
d 7) [2053] |
CXCL11
(CXCL11, O14625)
(Selective) (pK
i 10.4–10.5) [734], CXCL10
(CXCL10, P02778)
(Selective) (pK
i 7.8–9.8) [734, 2006], CXCL9 (CXCL9, Q07325)
(Selective) (pK
i 7.3–8.3) [734, 2006] |
Agonists |
vCXCL1
(pIC50 7.4) [1158], HIV‐1 matrix protein
p17 (pK
d 5.7) [602] |
vCXCL1
(pIC50 8.2) [1158], HIV‐1 matrix protein
p17 (pK
d 6.9) [602] |
– |
Selective
agonists |
– |
– |
– |
Endogenous
antagonists |
– |
– |
CCL11 (CCL11, P51671)
(Selective) (pK
i 7.2) [2006], CCL7 (CCL7, P80098)
(Selective) (pK
i 6.6) [2006] |
Antagonists |
– |
– |
– |
Selective
antagonists |
– |
navarixin
(pIC50 10.3) [78, 456], danirixin
(pIC50 7.9) [1285], SB 225002
(pIC50 7.7) [2016], elubirixin
(pIC50 7.7) [78], SX‐517
(pIC50 7.2) [1172] |
– |
Allosteric
modulators |
reparixin
(Negative) (pIC50 9) [142] |
reparixin
(Negative) (pIC50 6.4) [142] |
– |
Labelled
ligands |
[125I]CXCL8
(human) (Agonist) (pK
d 8.9–9.6) [675, 1584] |
[125I]CXCL8
(human) (Agonist) (pK
d 9–9.4) [675, 1584], [125I]CXCL1
(human) (Agonist), [125I]CXCL5
(human) (Agonist), [125I]CXCL7
(human) (Agonist) |
[125I]CXCL10
(human) (Agonist), [125I]CXCL11
(human) (Agonist) |
Comments |
Reports on the
expression of native CXCR1 by mouse leukocytes are not conclusive.
There are reports on the existence of mouse Cxcr1 and
on Cxcr1 knockout mice, but the distinct function of
the gene and of its knockout phenotype are unclear [118, 351, 1297, 1628, 1794]. |
– |
– |