Target Information
Target General Infomation | |||||
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Target ID |
T89988
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Former ID |
TTDC00122
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Target Name |
C-C chemokine receptor type 2
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Gene Name |
CCR2
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Synonyms |
C-C CKR-2; CC-CKR-2; CCR-2; Chemokine receptor CCR2B; MCP-1-R; Monocyte chemoattractant protein 1 receptor; CCR2
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Target Type |
Clinical Trial
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Disease | Arteriosclerosis [ICD9: 440; ICD10: I70] | ||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Arthritis [ICD9: 710-719; ICD10: M00-M25] | |||||
Atherosclerosis [ICD9: 414.0, 440; ICD10: I70] | |||||
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47] | |||||
Diabetic nephropathy [ICD9: 250.4; ICD10: E11.21] | |||||
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25] | |||||
Multiple scierosis [ICD9: 340; ICD10: G35] | |||||
Metastatic cancer; Multiple scierosis [ICD9:140-199, 140-229, 210-229, 340; ICD10: D10-D36, D3A, G35] | |||||
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0] | |||||
Obese insulin-resistant disorders; Rheumatoid arthritis [ICD9:250, 710-719, 714; ICD10: E11, M05-M06] | |||||
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06] | |||||
Function |
Receptor for the CCL2, CCL7 and CCL13 chemokines. Transduces a signal by increasing intracellular calcium ion levels. Alternative coreceptor with CD4 for HIV-1 infection.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T89988
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UniProt ID | |||||
Sequence |
MLSTSRSRFIRNTNESGEEVTTFFDYDYGAPCHKFDVKQIGAQLLPPLYSLVFIFGFVGN
MLVVLILINCKKLKCLTDIYLLNLAISDLLFLITLPLWAHSAANEWVFGNAMCKLFTGLY HIGYFGGIFFIILLTIDRYLAIVHAVFALKARTVTFGVVTSVITWLVAVFASVPGIIFTK CQKEDSVYVCGPYFPRGWNNFHTIMRNILGLVLPLLIMVICYSGILKTLLRCRNEKKRHR AVRVIFTIMIVYFLFWTPYNIVILLNTFQEFFGLSNCESTSQLDQATQVTETLGMTHCCI NPIIYAFVGEKFRSLFHIALGCRIAPLQKPVCGGPGVRPGKNVKVTTQGLLDGRGKGKSI GRAPEASLQDKEGA |
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Structure |
1KAD; 1KP1
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Drugs and Mode of Action | |||||
Drug(s) | BMS-813160 | Drug Info | Phase 2 | Diabetic nephropathy | [524165] |
CCX-140 | Drug Info | Phase 2 | Diabetic nephropathy | [547696] | |
MK-0812 | Drug Info | Phase 2 | Multiple scierosis | [521746] | |
MLN1202 | Drug Info | Phase 2 | Metastatic cancer; Multiple scierosis | [537520] | |
CCX872 | Drug Info | Phase 1 | Diabetic nephropathy | [525071] | |
OPL-CCL2-LPM | Drug Info | Phase 1 | Arthritis | [548903] | |
MCP-1 | Drug Info | Preclinical | Rheumatoid arthritis | [536223] | |
RS-504393 | Drug Info | Preclinical | Chronic obstructive pulmonary disease | [536223], [542757] | |
AZD-2423 | Drug Info | Discontinued in Phase 2 | Chronic obstructive pulmonary disease | [523197], [542770] | |
INCB3284 | Drug Info | Discontinued in Phase 2 | Obese insulin-resistant disorders; Rheumatoid arthritis | [547666] | |
CCX915 | Drug Info | Discontinued in Phase 1 | Multiple scierosis | [549358] | |
INCB8696 | Drug Info | Discontinued in Phase 1 | Multiple scierosis | [548303] | |
AZD-6942 | Drug Info | Terminated | Rheumatoid arthritis | [547438] | |
INCB3344 | Drug Info | Terminated | Arteriosclerosis | [542721], [549359] | |
SB-282241 | Drug Info | Terminated | Inflammatory disease | [526712], [542764] | |
Inhibitor | (R)-3-(1'-Adamantanecarbonyl)amino-caprolactam | Drug Info | [530113] | ||
(S)-3-(1'-Adamantanecarbonyl)amino-caprolactam | Drug Info | [530113] | |||
(S)-3-(2',2'-Dimethyl-propionyl)amino-caprolactam | Drug Info | [530113] | |||
CCX872 | Drug Info | [551637] | |||
NSC-651016 | Drug Info | [534649] | |||
Antagonist | AZD-2423 | Drug Info | [550850] | ||
AZD-6942 | Drug Info | [550879] | |||
BMS-A | Drug Info | [543887] | |||
CCX-140 | Drug Info | [533233] | |||
CCX915 | Drug Info | [550191] | |||
GSK Compound 34 | Drug Info | [543887] | |||
GSK-1344386B | Drug Info | [543887] | |||
INCB-10820 | Drug Info | [543887] | |||
INCB3284 | Drug Info | [550211] | |||
INCB3344 | Drug Info | [531362] | |||
INCB8696 | Drug Info | [551022] | |||
MCP-1 | Drug Info | [536223] | |||
MK-0812 | Drug Info | [530515] | |||
MLN1202 | Drug Info | [536223] | |||
RS-102895 | Drug Info | [525750] | |||
RS-136270 | Drug Info | [525750] | |||
RS-504393 | Drug Info | [536223], [536550] | |||
SB-282241 | Drug Info | [550879] | |||
Teijin-lead_cmp_5 | Drug Info | [526712] | |||
viral macrophage inflammatory protein-II | Drug Info | [534456] | |||
Modulator | BMS-813160 | Drug Info | [531630] | ||
OPL-CCL2-LPM | Drug Info | [544075] | |||
RAP-103 | Drug Info | [543887] | |||
RAP-310 | Drug Info | [543887] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Cytokine-cytokine receptor interaction | ||||
Chemokine signaling pathway | |||||
NetPath Pathway | TCR Signaling Pathway | ||||
IL2 Signaling Pathway | |||||
TGF_beta_Receptor Signaling Pathway | |||||
Leptin Signaling Pathway | |||||
RANKL Signaling Pathway | |||||
PANTHER Pathway | Inflammation mediated by chemokine and cytokine signaling pathway | ||||
Reactome | Beta defensins | ||||
Chemokine receptors bind chemokines | |||||
G alpha (i) signalling events | |||||
WikiPathways | GPCRs, Class A Rhodopsin-like | ||||
Defensins | |||||
Spinal Cord Injury | |||||
Peptide GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 521746 | ClinicalTrials.gov (NCT00239655) A Study to Assess the Effects of MK0812 on Disease Activity in Patients With Relapsing-Remitting Multiple Sclerosis as Measured by Magnetic Resonance Imaging (MRI). U.S. National Institutes of Health. | ||||
Ref 523197 | ClinicalTrials.gov (NCT01215279) AZD2423 Safety and Tolerability Study in Patients With Moderate and Severe Chronic Obstructive Pulmonary Disease(COPD). 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 525071 | ClinicalTrials.gov (NCT02345408) Phase 1b Study of CCX872-B in Patients With Pancreatic Adenocarcinoma. U.S. National Institutes of Health. | ||||
Ref 526712 | CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. J Med Chem. 2003 Sep 11;46(19):4070-86. | ||||
Ref 536223 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. | ||||
Ref 537520 | Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Jun 24. | ||||
Ref 542721 | (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: 777). | ||||
Ref 542757 | (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: 781). | ||||
Ref 542764 | (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: 782). | ||||
Ref 542770 | (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: 7825). | ||||
Ref 547438 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016328) | ||||
Ref 547666 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018258) | ||||
Ref 547696 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018498) | ||||
Ref 548303 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024340) | ||||
Ref 548903 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030092) | ||||
Ref 525750 | J Biol Chem. 2000 Aug 18;275(33):25562-71.Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helicalbundle. | ||||
Ref 526712 | CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. J Med Chem. 2003 Sep 11;46(19):4070-86. | ||||
Ref 530113 | J Med Chem. 2009 Jun 11;52(11):3591-5.Highly potent, orally available anti-inflammatory broad-spectrum chemokine inhibitors. | ||||
Ref 530515 | Assessment of chemokine receptor function on monocytes in whole blood: In vitro and ex vivo evaluations of a CCR2 antagonist. J Immunol Methods. 2010 Jan 31;352(1-2):101-10. | ||||
Ref 531362 | Discovery of ((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methanone, PF-4254196, a CCR2 antagonist with an improved cardiovascular profile. Bioorg Med Chem Lett. 2011 May 1;21(9):2626-30. | ||||
Ref 531630 | A dual CCR2/CCR5 chemokine antagonist, BMS-813160. Expert Opin Ther Pat. 2011 Dec;21(12):1919-24. | ||||
Ref 533233 | Present and future in the treatment of diabetic kidney disease. J Diabetes Res. 2015;2015:801348. | ||||
Ref 534456 | A broad-spectrum chemokine antagonist encoded by Kaposi's sarcoma-associated herpesvirus. Science. 1997 Sep 12;277(5332):1656-9. | ||||
Ref 534649 | J Med Chem. 1998 Jun 18;41(13):2184-93.Inhibition of in vitro and in vivo HIV replication by a distamycin analogue that interferes with chemokine receptor function: a candidate for chemotherapeutic and microbicidal application. | ||||
Ref 536223 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. | ||||
Ref 536550 | Beneficial or detrimental effects of carotenoids contained in food: cell culture models. Mini Rev Med Chem. 2007 Nov;7(11):1120-8. | ||||
Ref 543887 | (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. (Target id: 59). | ||||
Ref 544075 | Selective CCR2-targeted macrophage depletion ameliorates experimental mesangioproliferative glomerulonephritis. Clin Exp Immunol. 2009 February; 155(2): 295-303. | ||||
Ref 550191 | Marketed and experimental medicines for the treatment of multiple sclerosis. The Association of the British Pharmaceutical Industry. 2009. |
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