Target Information

Target General Infomation
Target ID
T16016
Former ID
TTDC00215
Target Name
C-C chemokine receptor type 1
Gene Name
CCR1
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
Target Type
Clinical Trial
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T16016
UniProt ID
P32246
Sequence
METPNTTEDYDTTTEFDYGDATPCQKVNERAFGAQLLPPLYSLVFVIGLVGNILVVLVLV
QYKRLKNMTSIYLLNLAISDLLFLFTLPFWIDYKLKDDWVFGDAMCKILSGFYYTGLYSE
IFFIILLTIDRYLAIVHAVFALRARTVTFGVITSIIIWALAILASMPGLYFSKTQWEFTH
HTCSLHFPHESLREWKLFQALKLNLFGLVLPLLVMIICYTGIIKILLRRPNEKKSKAVRL
IFVIMIIFFLFWTPYNLTILISVFQDFLFTHECEQSRHLDLAVQVTEVIAYTHCCVNPVI
YAFVGERFRKYLRQLFHRRVAVHLVKWLPFLSVDRLERVSSTSPSTGEHELSAGF
Structure
1Y5D
Drugs and Mode of Action
Drug(s) BMS-817399 Drug Info Phase 2 Rheumatoid arthritis [523564]
CCX-354 Drug Info Phase 2 Autoimmune diabetes [523255]
GSK2941266 Drug Info Phase 2 Rheumatoid arthritis [548754]
AVE1701 Drug Info Phase 1 Rheumatoid arthritis [536651]
AZD4818 Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease [548470]
MLN3897 Drug Info Discontinued in Phase 2 Rheumatoid arthritis [536651]
COSALANE Drug Info Terminated Discovery agent [545653]
Inhibitor A-987306 Drug Info [529789]
COSALANE Drug Info [525947]
Cosalane derivative Drug Info [525947]
Antagonist AVE1701 Drug Info [536651]
AZD4818 Drug Info [550288]
BX 471 Drug Info [534976]
CCX-354 Drug Info [531908]
MLN3897 Drug Info [536651]
Modulator BMS-817399 Drug Info [532913]
GSK2941266 Drug Info [531908]
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 523255ClinicalTrials.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 523564ClinicalTrials.gov (NCT01404585) Proof-of-Concept Study With BMS-817399 to Treat Moderate to Severe Rheumatoid Arthritis. U.S. National Institutes of Health.
Ref 536651Emerging drugs for rheumatoid arthritis. Expert Opin Emerg Drugs. 2008 Mar;13(1):175-96.
Ref 545653Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004038)
Ref 548470Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025769)
Ref 548754Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028338)
Ref 525947Bioorg Med Chem Lett. 2001 Jan 8;11(1):59-62.Inhibition of RANTES/CCR1-mediated chemotaxis by cosalane and related compounds.
Ref 529789J 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 531908Chemokine 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 532913Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis. J Med Chem. 2014 Sep 25;57(18):7550-64.
Ref 534976Identification 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 536651Emerging drugs for rheumatoid arthritis. Expert Opin Emerg Drugs. 2008 Mar;13(1):175-96.
Ref 550288Clinical pipeline report, company report or official report of AstraZeneca (2009).

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