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. 2015 Dec 9;172(24):5744–5869. doi: 10.1111/bph.13348
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].