Therapeutic Targets Database
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TTD Target ID: TTDS00326

Target Information
NameC-C chemokine receptor type 5    
Type of targetSuccessful target    
SynonymsC-C CKR-5    
CC-CKR-5    
CCR-5    
CCR5    
CD195 antigen    
CHEMR13    
Chemokine receptor CCR5    
HIV-1 fusion co-receptor    
HIV-1 fusion coreceptor    
DiseaseHuman immunodeficiency virus [HIV] disease
[ICD9: 279.3   ICD10: D84.9]
[1][2]
Drug(s)MaravirocApprovedHIV infection[3][4][5]
MaravirocPhase IIIChronic obstructive pulmonary disease[6][7]
VicrivirocPhase IIIHIV Infection[8]
INCB9471Phase IIa completedInfections[9]
PRO 140Phase II completedHIV Infection[10][1]
CenicrivirocPhase IIHIV-1 infection treatment
RAP101Phase IIHIV infection treatment
SCH-DPhase IIHIV Infection[10][1]
AZD8566Phase I completedChronic obstructive pulmonary disease; Rheumatoid arthritis[11]
Tak-220Phase IHIV-1[10]
AZD5672Discontinued in Phase IRheumatoid arthritis[11]
GW873140Terminated in Phase IIIHIV-1 Infection[12][10]
INCB15050Discontinued in Phase IHIV infection[13]
SCH-CDiscontinuedHIV Infection[10]
Sch-351125DiscontinuedHIV Infection[9]
TAK-779DiscontinuedHIV Infection[9][10]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayChemokine signaling pathway
Cytokine-cytokine receptor interaction
UniProt IDP51681
PDB Structure1ND8; 1NE0; 1OPN; 1OPT; 1OPW; 2L87; 2RLL; 2RRS.    
FunctionReceptor for a c-c type chemokine. Binds to MIP-1-alpha, MIP-1-beta and rantes and subsequently transduces a signal by increasing the intracellular calcium ions level. May play a role in the control of granulocytic lineage proliferation or differentiation.    
SequenceMDYQVSSPIYDINYYTSEPCQKINVKQIAARLLPPLYSLVFIFGFVGNMLVILILINCKR LKSMTDIYLLNLAISDLFFLLTVPFWAHYAAAQWDFGNTMCQLLTGLYFIGFFSGIFFII LLTIDRYLAVVHAVFALKARTVTFGVVTSVITWVVAVFASLPGIIFTRSQKEGLHYTCSS HFPYSQYQFWKNFQTLKIVILGLVLPLLVMVICYSGILKTLLRCRNEKKRHRAVRLIFTI MIVYFLFWAPYNIVLLLNTFQEFFGLNNCSSSNRLDQAMQVTETLGMTHCCINPIIYAFV GEKFRNYLLVFFQKHIAKRFCKCCSIFQQEAPERASSVYTRSTGEQEISVGL
Related US Patent6,387,930
6,391,865
6,476,062
6,562,978
6,602,885
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor (2-[14]
4- (2-[15]
ANIBAMINE[16]
GT-1282,   NIBR-1282[17]
N- (2-[14]
NIFEVIROC[18]
SCH-210971[19]
TAK-652[20]
UK-427857[21]
VARIECOLIN[22]
AntagonistAZD5672[11]
AZD8566[11]
E-913[9]
INCB15050[13]
INCB9471[9]
Maraviroc[3][4][5]
Maraviroc[6][7]
SCH 351125[1]
SCH-D[10][1]
Sch-351125[9]
TAK-779[9][10]
Vicriviroc[8]
AntibodyAnti-CCR5 antibodies[1]
PRO 140[10][1]
BinderGW873140[12][10]
SCH-C[10]
Tak-220[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1HIV entry inhibitors in clinical development. Curr Opin Pharmacol. 2002 Oct;2(5):523-8. To Reference
Ref 2Three-dimensional quantitative structure-activity relationship analyses of piperidine-based CCR5 receptor antagonists. Bioorg Med Chem. 2004 Jan 15;12(2):489-99. To Reference
Ref 3Rapamycin enhances aplaviroc anti-HIV activity: implications for the clinical development of novel CCR5 antagonists. Antiviral Res. 2009 Jul;83(1):86-9. Epub 2009 Mar 9. To Reference
Ref 4Tyrosine sulfation of the amino terminus of CCR5 facilitates HIV-1 entry. Cell. 1999 Mar 5;96(5):667-76. To Reference
Ref 5Molecular cloning and functional expression of a new human CC-chemokine receptor gene. Biochemistry. 1996 Mar 19;35(11):3362-7. To Reference
Ref 6Maraviroc: a new CCR5 antagonist. Expert Rev Anti Infect Ther. 2009 Feb;7(1):9-19. To Reference
Ref 7Pfizer. Product Development Pipeline. March 31 2009. To Reference
Ref 8HIV entry: new insights and implications for patient management. Curr Opin Infect Dis. 2009 Feb;22(1):35-42. To Reference
Ref 9Species selectivity of small-molecular antagonists for the CCR5 chemokine receptor. Int Immunopharmacol. 2007 Dec 5;7(12):1528-34. Epub 2007 Aug 14. To Reference
Ref 10Progress in targeting HIV-1 entry. Drug Discov Today. 2005 Aug 15;10(16):1085-94. To Reference
Ref 11AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 12In vitro and clinical investigation of the relationship between CCR5 receptor occupancy and anti-HIV activity of Aplaviroc. J Clin Pharmacol. 2008 Oct;48(10):1179-88. Epub 2008 Aug 1. To Reference
Ref 13Incyte. Product Development Pipeline. 2009. To Reference
Ref 14Bioorg Med Chem Lett. 2007 Apr 1;17(7):1883-7. Epub 2007 Jan 25.CCR5 receptor antagonists: discovery and SAR of novel 4-hydroxypiperidine derivatives. To Reference
Ref 15Bioorg Med Chem Lett. 2007 Jan 1;17(1):231-4. Epub 2006 Nov 1.CCR5 receptor antagonists: discovery and SAR study of guanylhydrazone derivatives. To Reference
Ref 16J Nat Prod. 2004 Jun;67(6):1036-8.Isolation and structure of antagonists of chemokine receptor (CCR5). To Reference
Ref 17Bioorg Med Chem Lett. 2008 Mar 15;18(6):2000-5. Epub 2008 Feb 2.Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo. To Reference
Ref 18Bioorg Med Chem Lett. 2010 Sep 1;20(17):5334-6. Epub 2010 May 19.Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents. To Reference
Ref 19J Nat Prod. 2006 Jul;69(7):1025-8.Chemokine receptor CCR-5 inhibitors produced by Chaetomium globosum. To Reference
Ref 20J Med Chem. 2006 Mar 23;49(6):2037-48.Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety. To Reference
Ref 21J Med Chem. 2005 Mar 10;48(5):1297-313.New approaches toward anti-HIV chemotherapy. To Reference
Ref 22J Nat Prod. 2004 Oct;67(10):1681-4.Inhibition of the human chemokine receptor CCR5 by variecolin and variecolol and isolation of four new variecolin analogues, emericolins A-D, from Emericella aurantiobrunnea. To Reference



 

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