Target Information
Target General Infomation | |||||
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Target ID |
T09960
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Former ID |
TTDS00326
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Target Name |
C-C chemokinereceptor type 5
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Gene Name |
CCR5
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Synonyms |
C-C CKR-5; CC-CKR-5; CCR-5; CD195 antigen; CHEMR13; Chemokine receptor CCR5; HIV-1 fusion co-receptor; HIV-1 fusion coreceptor; CCR5
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Target Type |
Successful
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Disease | Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47] | ||||
Chronic obstructive pulmonary disease; Rheumatoid arthritis [ICD9: 460-519, 490-492, 494-496, 710-719, 714; ICD10: J00-J99, J40-J44, J47, M00-M25, M05-M06] | |||||
Diabetic nephropathy [ICD9: 250.4; ICD10: E11.21] | |||||
Human immunodeficiency virus infection [ICD9: 279.3; ICD10: B20-B26] | |||||
HIV-1 infection [ICD9: 001-139, 042; ICD10: B20-B24] | |||||
Infections [ICD9: 001-139; ICD10: A00-B99] | |||||
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06] | |||||
Transplant rejection [ICD9: 279.5, 996; ICD10: D89.8, T86] | |||||
Function |
Receptor 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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T09960
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UniProt ID | |||||
Sequence |
MDYQVSSPIYDINYYTSEPCQKINVKQIAARLLPPLYSLVFIFGFVGNMLVILILINCKR
LKSMTDIYLLNLAISDLFFLLTVPFWAHYAAAQWDFGNTMCQLLTGLYFIGFFSGIFFII LLTIDRYLAVVHAVFALKARTVTFGVVTSVITWVVAVFASLPGIIFTRSQKEGLHYTCSS HFPYSQYQFWKNFQTLKIVILGLVLPLLVMVICYSGILKTLLRCRNEKKRHRAVRLIFTI MIVYFLFWAPYNIVLLLNTFQEFFGLNNCSSSNRLDQAMQVTETLGMTHCCINPIIYAFV GEKFRNYLLVFFQKHIAKRFCKCCSIFQQEAPERASSVYTRSTGEQEISVGL |
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Drugs and Mode of Action | |||||
Drug(s) | Maraviroc | Drug Info | Approved | Human immunodeficiency virus infection | [529282], [536223], [542947] |
E-913 | Drug Info | Phase 3 | Human immunodeficiency virus infection | [521808], [540440] | |
Maraviroc | Drug Info | Phase 3 | Chronic obstructive pulmonary disease | [536223], [542947] | |
Vicriviroc | Drug Info | Phase 3 | Human immunodeficiency virus infection | [536833], [542952] | |
INCB9471 | Drug Info | Phase 2a | Infections | [548244] | |
BMS-813160 | Drug Info | Phase 2 | Diabetic nephropathy | [524165] | |
Cenicriviroc | Drug Info | Phase 2 | Human immunodeficiency virus infection | [533043], [542922] | |
GSK-706769 | Drug Info | Phase 2 | Human immunodeficiency virus infection | [522788] | |
INCB9471 | Drug Info | Phase 2 | Human immunodeficiency virus infection | [549860] | |
PF-232798 | Drug Info | Phase 2 | Human immunodeficiency virus infection | [531280] | |
PRO-140 | Drug Info | Phase 2 | Human immunodeficiency virus infection | [525183] | |
Cal-1 | Drug Info | Phase 1/2 | HIV-1 infection | [524138] | |
SB-728-T | Drug Info | Phase 1/2 | Human immunodeficiency virus infection | [523810] | |
CCR5 mab | Drug Info | Phase 1 | Human immunodeficiency virus infection | [544105] | |
INCB15050 | Drug Info | Phase 1 | Human immunodeficiency virus infection | [548427] | |
Tak-220 | Drug Info | Phase 1 | HIV-1 infection | [542915], [548134] | |
VCH-286 | Drug Info | Phase 1 | Human immunodeficiency virus infection | [531985] | |
GW873140 | Drug Info | Discontinued in Phase 3 | HIV-1 infection | [542944], [547670] | |
AZD8566 | Drug Info | Discontinued in Phase 1 | Chronic obstructive pulmonary disease; Rheumatoid arthritis | [548691] | |
SCH-C | Drug Info | Discontinued in Phase 1 | Human immunodeficiency virus infection | [542937], [547223] | |
AZD5672 | Drug Info | Terminated | Rheumatoid arthritis | [531058], [542666] | |
CCR5 receptor inhibitors | Drug Info | Terminated | Human immunodeficiency virus infection | [548211] | |
CCR5Qb | Drug Info | Terminated | Human immunodeficiency virus infection | [548077] | |
TAK-779 | Drug Info | Terminated | Transplant rejection | [542775], [547013] | |
Inhibitor | (2-(4-chlorobenzyloxy)-5-bromophenyl)methanamine | Drug Info | [528689] | ||
4-(2-(4-chlorobenzyloxy)-5-bromobenzyl)morpholine | Drug Info | [528511] | |||
ANIBAMINE | Drug Info | [527121] | |||
CMPD-167 | Drug Info | [540496] | |||
GT-1282 | Drug Info | [529307] | |||
N-(2-(4-chlorobenzyloxy)-5-bromobenzyl)ethanamine | Drug Info | [528689] | |||
SCH-210971 | Drug Info | [528341] | |||
VARIECOLIN | Drug Info | [527257] | |||
Antagonist | AZD5672 | Drug Info | [550288] | ||
AZD8566 | Drug Info | [550288] | |||
CCR5 receptor inhibitors | Drug Info | [529636] | |||
E-913 | Drug Info | [536516] | |||
GSK-706769 | Drug Info | [530181] | |||
INCB15050 | Drug Info | [551022] | |||
INCB9471 | Drug Info | [536516] | |||
Maraviroc | Drug Info | [534846], [537430], [537962] | |||
PF-232798 | Drug Info | [531280] | |||
PRO-140 | Drug Info | [531384] | |||
TAK-779 | Drug Info | [536143], [536516] | |||
VCH-286 | Drug Info | [531985] | |||
Vicriviroc | Drug Info | [537478] | |||
Modulator | BMS-813160 | Drug Info | [531630] | ||
Cal-1 | Drug Info | [533257] | |||
Cenicriviroc | Drug Info | [533043] | |||
NIFEVIROC | Drug Info | [531584] | |||
SB-728-T | Drug Info | [544423] | |||
Binder | GW873140 | Drug Info | [536143], [536797] | ||
SCH-C | Drug Info | [536143] | |||
Tak-220 | Drug Info | [536143] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Cytokine-cytokine receptor interaction | ||||
Chemokine signaling pathway | |||||
Endocytosis | |||||
Toxoplasmosis | |||||
Viral carcinogenesis | |||||
NetPath Pathway | TSLP Signaling Pathway | ||||
TCR Signaling Pathway | |||||
IL2 Signaling Pathway | |||||
PANTHER Pathway | Inflammation mediated by chemokine and cytokine signaling pathway | ||||
Pathway Interaction Database | IL12-mediated signaling events | ||||
Reactome | Binding and entry of HIV virion | ||||
Chemokine receptors bind chemokines | |||||
G alpha (i) signalling events | |||||
WikiPathways | TCR Signaling Pathway | ||||
GPCRs, Class A Rhodopsin-like | |||||
HIV Life Cycle | |||||
Peptide GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
GPCRs, Other | |||||
References | |||||
Ref 521808 | ClinicalTrials.gov (NCT00297076) Chemokine Coreceptor 5 (CCR5) Antagonist GW873140 In R5-Tropic Treatment-Experienced HIV-Infected Subjects. U.S. National Institutes of Health. | ||||
Ref 522788 | ClinicalTrials.gov (NCT00979771) A Study to Investigate the Ability of GSK706769 to Maintain Clinical Remission After Withdrawal of Enbrel in Rheumatoid Arthritis Patients. U.S. National Institutes of Health. | ||||
Ref 523810 | ClinicalTrials.gov (NCT01543152) Dose Escalation Study of Cyclophosphamide in HIV-Infected Subjects on HAART Receiving SB-728-T. U.S. National Institutes of Health. | ||||
Ref 524138 | ClinicalTrials.gov (NCT01734850) Safety Study of a Dual Anti-HIV Gene Transfer Construct to Treat HIV-1 Infection. U.S. National Institutes of Health. | ||||
Ref 524165 | ClinicalTrials.gov (NCT01752985) Study to Evaluate the Effects of BMS-813160 on Protein Loss in the Urine of Subjects With Type 2 Diabetes and Diabetic Kidney Disease. U.S. National Institutes of Health. | ||||
Ref 525183 | ClinicalTrials.gov (NCT02438345) PRO 140 for Human Immunodeficiency Virus. U.S. National Institutes of Health. | ||||
Ref 531058 | Preclinical and clinical investigation of a CCR5 antagonist, AZD5672, in patients with rheumatoid arthritis receiving methotrexate. Arthritis Rheum. 2010 Nov;62(11):3154-60. | ||||
Ref 531280 | An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: the discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-232798). J Med Chem. 2011 Jan 13;54(1):67-77. | ||||
Ref 531985 | The Continuing Evolution of HIV-1 Therapy: Identification and Development of Novel Antiretroviral Agents Targeting Viral and Cellular Targets. Mol Biol Int. 2012;2012:401965. | ||||
Ref 533043 | The dual CCR5 and CCR2 inhibitor cenicriviroc does not redistribute HIV into extracellular space: implications for plasma viral load and intracellular DNA decline. J Antimicrob Chemother. 2015 Mar;70(3):750-6. | ||||
Ref 536223 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. | ||||
Ref 540440 | (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: 3500). | ||||
Ref 542666 | (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: 7686). | ||||
Ref 542775 | (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: 783). | ||||
Ref 542915 | (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: 800). | ||||
Ref 542922 | (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: 801). | ||||
Ref 542937 | (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: 804). | ||||
Ref 542944 | (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: 805). | ||||
Ref 542947 | (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: 806). | ||||
Ref 542952 | (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: 807). | ||||
Ref 544105 | CCR5 Monoclonal Antibodies for HIV-1 Therapy. Curr Opin HIV AIDS. 2009 March; 4(2): 104-111. | ||||
Ref 547013 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012061) | ||||
Ref 547223 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014207) | ||||
Ref 547670 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018317) | ||||
Ref 548077 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021743) | ||||
Ref 548134 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022281) | ||||
Ref 548211 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023138) | ||||
Ref 548244 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023697) | ||||
Ref 548427 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025519) | ||||
Ref 527121 | J Nat Prod. 2004 Jun;67(6):1036-8.Isolation and structure of antagonists of chemokine receptor (CCR5). | ||||
Ref 527257 | J 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. | ||||
Ref 528341 | J Nat Prod. 2006 Jul;69(7):1025-8.Chemokine receptor CCR-5 inhibitors produced by Chaetomium globosum. | ||||
Ref 528511 | Bioorg Med Chem Lett. 2007 Jan 1;17(1):231-4. Epub 2006 Nov 1.CCR5 receptor antagonists: discovery and SAR study of guanylhydrazone derivatives. | ||||
Ref 528689 | Bioorg 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. | ||||
Ref 529307 | Bioorg 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. | ||||
Ref 529636 | Maraviroc: a CCR5-receptor antagonist for the treatment of HIV-1 infection. Clin Ther. 2008 Jul;30(7):1228-50. | ||||
Ref 531280 | An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: the discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-232798). J Med Chem. 2011 Jan 13;54(1):67-77. | ||||
Ref 531384 | Agonist-induced internalization of CC chemokine receptor 5 as a mechanism to inhibit HIV replication. J Pharmacol Exp Ther. 2011 Jun;337(3):655-62. | ||||
Ref 531584 | Determination of nifeviroc, a novel CCR5 antagonist: application to a pharmacokinetic study. J Pharm Biomed Anal. 2011 Nov 1;56(3):637-40. | ||||
Ref 531630 | A dual CCR2/CCR5 chemokine antagonist, BMS-813160. Expert Opin Ther Pat. 2011 Dec;21(12):1919-24. | ||||
Ref 531985 | The Continuing Evolution of HIV-1 Therapy: Identification and Development of Novel Antiretroviral Agents Targeting Viral and Cellular Targets. Mol Biol Int. 2012;2012:401965. | ||||
Ref 533043 | The dual CCR5 and CCR2 inhibitor cenicriviroc does not redistribute HIV into extracellular space: implications for plasma viral load and intracellular DNA decline. J Antimicrob Chemother. 2015 Mar;70(3):750-6. | ||||
Ref 533257 | Preclinical safety and efficacy of an anti-HIV-1 lentiviral vector containing a short hairpin RNA to CCR5 and the C46 fusion inhibitor. Mol Ther Methods Clin Dev. 2014 Feb 12;1:11. | ||||
Ref 534846 | Tyrosine sulfation of the amino terminus of CCR5 facilitates HIV-1 entry. Cell. 1999 Mar 5;96(5):667-76. | ||||
Ref 536516 | Species selectivity of small-molecular antagonists for the CCR5 chemokine receptor. Int Immunopharmacol. 2007 Dec 5;7(12):1528-34. Epub 2007 Aug 14. | ||||
Ref 536797 | In 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. | ||||
Ref 537430 | Rapamycin 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. | ||||
Ref 537478 | HIV entry: new insights and implications for patient management. Curr Opin Infect Dis. 2009 Feb;22(1):35-42. | ||||
Ref 537962 | Molecular cloning and functional expression of a new human CC-chemokine receptor gene. Biochemistry. 1996 Mar 19;35(11):3362-7. | ||||
Ref 540496 | (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: 3651). | ||||
Ref 544105 | CCR5 Monoclonal Antibodies for HIV-1 Therapy. Curr Opin HIV AIDS. 2009 March; 4(2): 104-111. | ||||
Ref 544423 | Gene Editing of CCR5 in Autologous CD4 T Cells of Persons Infected with HIV. N Engl J Med. 2014 March 6; 370(10): 901-910. |
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