Target Information
Target General Infomation | |||||
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Target ID |
T00884
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Former ID |
TTDC00190
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Target Name |
High affinity interleukin-8 receptor A
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Gene Name |
CXCR1
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Synonyms |
CDw128a; CXCR-1; IL-8 receptor type 1; IL-8R A; Interleukin-8 receptor A; CXCR1
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Target Type |
Clinical Trial
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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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T00884
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UniProt ID | |||||
Sequence |
MSNITDPQMWDFDDLNFTGMPPADEDYSPCMLETETLNKYVVIIAYALVFLLSLLGNSLV
MLVILYSRVGRSVTDVYLLNLALADLLFALTLPIWAASKVNGWIFGTFLCKVVSLLKEVN FYSGILLLACISVDRYLAIVHATRTLTQKRHLVKFVCLGCWGLSMNLSLPFFLFRQAYHP NNSSPVCYEVLGNDTAKWRMVLRILPHTFGFIVPLFVMLFCYGFTLRTLFKAHMGQKHRA MRVIFAVVLIFLLCWLPYNLVLLADTLMRTQVIQESCERRNNIGRALDATEILGFLHSCL NPIIYAFIGQNFRHGFLKILAMHGLVSKEFLARHRVTSYTSSSVNVSSNL |
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Structure |
1ILP; 1ILQ; 2LNL
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Drugs and Mode of Action | |||||
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 537129 | New 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 526980 | J Med Chem. 2004 Mar 11;47(6):1319-21.Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor. | ||||
Ref 527139 | Bioorg 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. |
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