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Compound class: Endogenous peptide in human, mouse or rat
Comment: The CXCL8 (IL-8) chemokine is upregulated at sites of inflammation where it promotes neutrophil infiltration and activation. It can form homodimers and heterodimers with CXCL4.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Bertini R, Allegretti M, Bizzarri C, Moriconi A, Locati M, Zampella G, Cervellera MN, Di Cioccio V, Cesta MC, Galliera E et al.. (2004)
Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury.
Proc Natl Acad Sci USA, 101 (32): 11791-6. [PMID:15282370]
2. Bozic CR, Gerard NP, von Uexkull-Guldenband C, Kolakowski Jr LF, Conklyn MJ, Breslow R, Showell HJ, Gerard C. (1994)
The murine interleukin 8 type B receptor homologue and its ligands. Expression and biological characterization.
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HIV-1 matrix protein p17 binds to the IL-8 receptor CXCR1 and shows IL-8-like chemokine activity on monocytes through Rho/ROCK activation.
Blood, 119 (10): 2274-83. [PMID:22262769]
4. Hall DA, Beresford IJ, Browning C, Giles H. (1999)
Signalling by CXC-chemokine receptors 1 and 2 expressed in CHO cells: a comparison of calcium mobilization, inhibition of adenylyl cyclase and stimulation of GTPgammaS binding induced by IL-8 and GROalpha.
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5. Lee J, Horuk R, Rice GC, Bennett GL, Camerato T, Wood WI. (1992)
Characterization of two high affinity human interleukin-8 receptors.
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6. Nishimoto-Kakiuchi A, Sato I, Nakano K, Ohmori H, Kayukawa Y, Tanimura H, Yamamoto S, Sakamoto Y, Nakamura G, Maeda A et al.. (2023)
A long-acting anti-IL-8 antibody improves inflammation and fibrosis in endometriosis.
Sci Transl Med, 15 (684): eabq5858. [PMID:36812343]
7. Wilson S, Wilkinson G, Milligan G. (2005)
The CXCR1 and CXCR2 receptors form constitutive homo- and heterodimers selectively and with equal apparent affinities.
J Biol Chem, 280 (31): 28663-74. [PMID:15946947]
8. Wu L, Ruffing N, Shi X, Newman W, Soler D, Mackay CR, Qin S. (1996)
Discrete steps in binding and signaling of interleukin-8 with its receptor.
J Biol Chem, 271 (49): 31202-9. [PMID:8940121]