Target Information

Target General Infomation
Target ID
T00884
Former ID
TTDC00190
Target Name
High affinity interleukin-8 receptor A
Gene Name
CXCR1
Synonyms
CDw128a; CXCR-1; IL-8 receptor type 1; IL-8R A; Interleukin-8 receptor A; CXCR1
Target Type
Clinical Trial
Disease Gout [ICD9: 274.00274.1274.8274.9; ICD10: M10]
Ischemia-reperfusion injury; Lung transplantation; Graft rejection in heart transplantation [ICD9: 996, 996.84; ICD10: T86, T86.81]
Function
Receptor to interleukin-8, which is a powerful neutrophils chemotactic factor. Binding of il-8 to the receptor causes activation of neutrophils. This response is mediated via a g-protein that activate a phosphatidylinositol-calcium second messenger system.
BioChemical Class
GPCR rhodopsin
Target Validation
T00884
UniProt ID
P25024
Sequence
MSNITDPQMWDFDDLNFTGMPPADEDYSPCMLETETLNKYVVIIAYALVFLLSLLGNSLV
MLVILYSRVGRSVTDVYLLNLALADLLFALTLPIWAASKVNGWIFGTFLCKVVSLLKEVN
FYSGILLLACISVDRYLAIVHATRTLTQKRHLVKFVCLGCWGLSMNLSLPFFLFRQAYHP
NNSSPVCYEVLGNDTAKWRMVLRILPHTFGFIVPLFVMLFCYGFTLRTLFKAHMGQKHRA
MRVIFAVVLIFLLCWLPYNLVLLADTLMRTQVIQESCERRNNIGRALDATEILGFLHSCL
NPIIYAFIGQNFRHGFLKILAMHGLVSKEFLARHRVTSYTSSSVNVSSNL
Structure
1ILP; 1ILQ; 2LNL
Drugs and Mode of Action
Drug(s) Reparixin Drug Info Phase 2 Ischemia-reperfusion injury; Lung transplantation; Graft rejection in heart transplantation [537129], [543171]
INDOPROFEN Drug Info Withdrawn from market Gout [551871]
R-KETOPROFEN Drug Info Discontinued in Phase 2 Discovery agent [546255]
Inhibitor (R)-2-(4-Isobutyl-phenyl)-N-methoxy-propionamide Drug Info [527602]
(R)-2-(4-Isobutyl-phenyl)-propionamide Drug Info [527602]
(R)-3-(4-Isobutyl-phenyl)-butan-2-one Drug Info [527602]
(R)-N-Hydroxy-2-(4-isobutyl-phenyl)-propionamide Drug Info [527602]
1-(2-Bromo-phenyl)-3-(2,4-dihydroxy-phenyl)-urea Drug Info [527139]
1-(2-hydroxy-4-nitrophenyl)-3-phenylurea Drug Info [526980]
2-(3-Isobutyl-phenyl)-propionic acid Drug Info [527602]
2-(3-Isopropyl-phenyl)-propionic acid Drug Info [527602]
2-[3-(1-Hydroxy-propyl)-phenyl]-propionic acid Drug Info [527602]
2-[3-(1-Phenyl-ethyl)-phenyl]-propionic acid Drug Info [527602]
2-[3-(2-Methyl-butyl)-phenyl]-propionic acid Drug Info [527602]
IBUPROPHEN Drug Info [527602]
INDOPROFEN Drug Info [527602]
R-KETOPROFEN Drug Info [527602]
RAPARIXIN Drug Info [527602]
Agonist Il-8((3-73))K11R Drug Info [535238]
Modulator Reparixin Drug Info
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Cytokine-cytokine receptor interaction
Chemokine signaling pathway
Endocytosis
Epithelial cell signaling in Helicobacter pylori infection
NetPath Pathway IL2 Signaling Pathway
PANTHER Pathway Inflammation mediated by chemokine and cytokine signaling pathway
Interleukin signaling pathway
Pathway Interaction Database IL8- and CXCR1-mediated signaling events
Reactome Chemokine receptors bind chemokines
G alpha (i) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Differentiation Pathway
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 537129New developments in immunosuppressive therapy for heart transplantation. Expert Opin Emerg Drugs. 2009 Mar;14(1):1-21.
Ref 543171(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8498).
Ref 546255Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007136)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 526980J Med Chem. 2004 Mar 11;47(6):1319-21.Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor.
Ref 527139Bioorg Med Chem Lett. 2004 Aug 16;14(16):4307-11.Synthesis and structure-activity relationships of 3,5-diarylisoxazoles and 3,5-diaryl-1,2,4-oxadiazoles, novel classes of small molecule interleukin-8(IL-8) receptor antagonists.
Ref 527602J Med Chem. 2005 Jun 30;48(13):4312-31.2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.
Ref 535238Il-8((3-73))K11R is a high affinity agonist of the neutrophil CXCR1 and CXCR2. Biochem Biophys Res Commun. 2001 Aug 24;286(3):595-600.

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