Therapeutic Targets Database
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TTD Target ID: TTDC00087

Target Information
NameHigh affinity interleukin-8 receptor B    
Type of targetClinical trial target    
SynonymsCDw128b    
CXCR-2    
GRO/MGSA receptor    
IL-8 receptor type 2    
IL-8R B    
Interleukin-8 receptor B    
DiseaseAcute respiratory distress syndrome
[ICD9: 518.5, 518.82   ICD10: J80]
[1]
Asthma
[ICD9: 493   ICD10: J45]
[1]
Chronic Obstructive Pulmonary Disease (COPD)
[ICD9: 490-492, 494-496   ICD10: J40-J44, J47]
[2]
Colorectal cancer
[ICD9: 153, 154   ICD10: C18-C21]
[3]
Lung injury[1]
Drug(s)ReparixinPhase II completedIschemia-Reperfusion Injury; Lung Transplantation; Graft rejection in heart transplantation[4]
AZD5069Phase IIAsthma
AZD5069Phase IICOPD
SB-656933Phase IIChronic obstructive pulmonary disease[5]
SB-656933Phase IICystic fibrosis & COPD[6]
SCH-527123Phase IIChronic obstructive pulmonary disease[7]
PS-938285Phase I completedChronic Obstructive Pulmonary Disease[2]
1325756Phase ICOPD
SB-265610Discontinued in Phase IChronic obstructive pulmonary disease[5]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayChemokine signaling pathway
Cytokine-cytokine receptor interaction
Epithelial cell signaling in Helicobacter pylori
UniProt IDP25025
FunctionReceptor 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.    
SequenceMEDFNMESDSFEDFWKGEDLSNYSYSSTLPPFLLDAAPCEPESLEINKYFVVIIYALVFL LSLLGNSLVMLVILYSRVGRSVTDVYLLNLALADLLFALTLPIWAASKVNGWIFGTFLCK VVSLLKEVNFYSGILLLACISVDRYLAIVHATRTLTQKRYLVKFICLSIWGLSLLLALPV LLFRRTVYSSNVSPACYEDMGNNTANWRMLLRILPQSFGFIVPLLIMLFCYGFTLRTLFK AHMGQKHRAMRVIFAVVLIFLLCWLPYNLVLLADTLMRTQVIQETCERRNHIDRALDATE ILGILHSCLNPLIYAFIGQKFRHGLLKILAIHGLISKDSLPKDSRPSFVGSSSGHTSTTL
Target ValidationClick to Find Target Validation Information.    
Inhibitor (R)-2-[8]
(R)-2-[8]
(R)-3-[8]
(R)-N-Hydroxy-2-[8]
1- (2-Hydroxy-3-nitro-phenyl)-3-phenyl-urea[9]
1- (2-Hydroxy-5-nitro-phenyl)-3-phenyl-urea[9]
1- (2-bromophenyl)-3-[10]
1- (2-hydroxy-4-nitrophenyl)-3-phenylurea[10]
1- (3-cyano-2-hydroxyphenyl)-3-phenylurea[10]
1- (4-cyano-2-hydroxyphenyl)-3-phenylurea[10]
1- (5-chloro-2-hydroxy-4-nitrophenyl)-3-phenylurea[10]
2- (3-Isobutyl-phenyl)-propionic acid[8]
2- (3-Isopropyl-phenyl)-propionic acid[8]
2-[3- (1-Hydroxy-propyl)-phenyl]-propionic acid[8]
2-[3- (1-Phenyl-ethyl)-phenyl]-propionic acid[8]
2-[3- (2-Methyl-butyl)-phenyl]-propionic acid[8]
5- (pentylthio)thiazolo[4,5-d]pyrimidin-7-ol[11]
IBUPROPHEN[8]
INDOPROFEN[8]
R-KETOPROFEN[8]
RAPARIXIN[8]
AgonistIl-8 ([12]
AntagonistN- (3-[13]
PS-938285[2]
Reparixin[4]
SB 225002[1]
SB 265610[1]
SB 272844[14]
SB-225002[5]
SB-265610[5]
SB-332235[5]
SB-656933[6]
SB-656933[5]
SCH-527123[7]
MultitargetReparixin[4]
SCH-527123[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Interleukin-8 receptor antagonists in pulmonary diseases. Curr Opin Pharmacol. 2001 Jun;1(3):242-7. To Reference
Ref 2CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference
Ref 3Angiogenic effects of interleukin 8 (CXCL8) in human intestinal microvascular endothelial cells are mediated by CXCR2. J Biol Chem. 2003 Mar 7;278(10):8508-15. Epub 2002 Dec 20. To Reference
Ref 4New developments in immunosuppressive therapy for heart transplantation. Expert Opin Emerg Drugs. 2009 Mar;14(1):1-21. To Reference
Ref 5Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. To Reference
Ref 6GSK. Product Development Pipeline. February 2009. To Reference
Ref 7Emerging drugs in chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2009 Mar;14(1):181-94. To Reference
Ref 8J Med Chem. 2005 Jun 30;48(13):4312-31.2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors. To Reference
Ref 9J Med Chem. 2004 Mar 11;47(6):1319-21.Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor. To Reference
Ref 10Bioorg Med Chem Lett. 2007 Mar 15;17(6):1713-7. Epub 2006 Dec 23.Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor. To Reference
Ref 11Bioorg Med Chem Lett. 2006 Feb 15;16(4):960-3. Epub 2005 Nov 15.Hit-to-Lead studies: the discovery of potent, orally bioavailable thiazolopyrimidine CXCR2 receptor antagonists. To Reference
Ref 12Il-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. To Reference
Ref 13A potent and selective nonpeptide antagonist of CXCR2 inhibits acute and chronic models of arthritis in the rabbit. J Immunol. 2002 Dec 1;169(11):6435-44. To Reference
Ref 14The selective CXCR2 antagonist SB272844 blocks interleukin-8 and growth-related oncogene-alpha-mediated inhibition of spontaneous neutrophil apoptosis. Pulm Pharmacol Ther. 2002;15(2):103-10. To Reference



 

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