Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T16016
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| Former ID |
TTDC00215
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| Target Name |
C-C chemokine receptor type 1
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| Gene Name |
CCR1
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| Synonyms |
C-C CKR-1; CC-CKR-1; CCR-1; Chemokine receptor CCR1; HM145; LD78 receptor; MIP-1alpha-R; Macrophage inflammatory protein-1 alpha receptor; RANTES-R; CCR1
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| Target Type |
Clinical Trial
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| Disease | Autoimmune diabetes [ICD10: E08-E13] | ||||
| Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47] | |||||
| Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06] | |||||
| Function |
Receptor for a C-C type chemokine.Binds to MIP-1-alpha, MIP-1-delta, RANTES, and MCP-3 and, less efficiently, to MIP-1- beta or MCP-1 and subsequently transduces a signal by increasing the intracellular calcium ions level. Responsible for affecting stem cell proliferation.
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| BioChemical Class |
GPCR rhodopsin
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| Target Validation |
T16016
|
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| UniProt ID | |||||
| Sequence |
METPNTTEDYDTTTEFDYGDATPCQKVNERAFGAQLLPPLYSLVFVIGLVGNILVVLVLV
QYKRLKNMTSIYLLNLAISDLLFLFTLPFWIDYKLKDDWVFGDAMCKILSGFYYTGLYSE IFFIILLTIDRYLAIVHAVFALRARTVTFGVITSIIIWALAILASMPGLYFSKTQWEFTH HTCSLHFPHESLREWKLFQALKLNLFGLVLPLLVMIICYTGIIKILLRRPNEKKSKAVRL IFVIMIIFFLFWTPYNLTILISVFQDFLFTHECEQSRHLDLAVQVTEVIAYTHCCVNPVI YAFVGERFRKYLRQLFHRRVAVHLVKWLPFLSVDRLERVSSTSPSTGEHELSAGF |
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| Structure |
1Y5D
|
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| Drugs and Mode of Action | |||||
| Drug(s) | BMS-817399 | Drug Info | Phase 2 | Rheumatoid arthritis | [1] |
| CCX-354 | Drug Info | Phase 2 | Autoimmune diabetes | [2] | |
| GSK2941266 | Drug Info | Phase 2 | Rheumatoid arthritis | [3] | |
| AVE1701 | Drug Info | Phase 1 | Rheumatoid arthritis | [4] | |
| AZD4818 | Drug Info | Discontinued in Phase 2 | Chronic obstructive pulmonary disease | [5] | |
| MLN3897 | Drug Info | Discontinued in Phase 2 | Rheumatoid arthritis | [4] | |
| COSALANE | Drug Info | Terminated | Discovery agent | [6] | |
| Inhibitor | A-987306 | Drug Info | [7] | ||
| COSALANE | Drug Info | [8] | |||
| Cosalane derivative | Drug Info | [8] | |||
| Antagonist | AVE1701 | Drug Info | [4] | ||
| AZD4818 | Drug Info | [9] | |||
| BX 471 | Drug Info | [10] | |||
| CCX-354 | Drug Info | [11] | |||
| MLN3897 | Drug Info | [4] | |||
| Modulator | BMS-817399 | Drug Info | [12] | ||
| GSK2941266 | Drug Info | [11] | |||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| KEGG Pathway | Cytokine-cytokine receptor interaction | ||||
| Chemokine signaling pathway | |||||
| NetPath Pathway | IL5 Signaling Pathway | ||||
| TCR Signaling Pathway | |||||
| IL2 Signaling Pathway | |||||
| TNFalpha Signaling Pathway | |||||
| Leptin Signaling Pathway | |||||
| PANTHER Pathway | Inflammation mediated by chemokine and cytokine signaling pathway | ||||
| Reactome | Chemokine receptors bind chemokines | ||||
| G alpha (i) signalling events | |||||
| WikiPathways | GPCRs, Class A Rhodopsin-like | ||||
| Peptide GPCRs | |||||
| GPCR ligand binding | |||||
| GPCR downstream signaling | |||||
| References | |||||
| REF 1 | ClinicalTrials.gov (NCT01404585) Proof-of-Concept Study With BMS-817399 to Treat Moderate to Severe Rheumatoid Arthritis. U.S. National Institutes of Health. | ||||
| REF 2 | ClinicalTrials.gov (NCT01242917) A Study to Evaluate the Safety and Efficacy of CCX354-C in Subjects With Rheumatoid Arthritis Partially Responsive to Methotrexate Therapy. U.S. National Institutes of Health. | ||||
| REF 3 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028338) | ||||
| REF 4 | Emerging drugs for rheumatoid arthritis. Expert Opin Emerg Drugs. 2008 Mar;13(1):175-96. | ||||
| REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025769) | ||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004038) | ||||
| REF 7 | J Med Chem. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. | ||||
| REF 8 | Bioorg Med Chem Lett. 2001 Jan 8;11(1):59-62.Inhibition of RANTES/CCR1-mediated chemotaxis by cosalane and related compounds. | ||||
| REF 9 | Clinical pipeline report, company report or official report of AstraZeneca (2009). | ||||
| REF 10 | Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem. 2000 Jun 23;275(25):19000-8. | ||||
| REF 11 | Chemokine receptor CCR1 antagonist CCX354-C treatment for rheumatoid arthritis: CARAT-2, a randomised, placebo controlled clinical trial. Ann Rheum Dis. 2013 Mar;72(3):337-44. | ||||
| REF 12 | Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis. J Med Chem. 2014 Sep 25;57(18):7550-64. | ||||
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