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 | |||||
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 523255 | 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 523564 | ClinicalTrials.gov (NCT01404585) Proof-of-Concept Study With BMS-817399 to Treat Moderate to Severe Rheumatoid Arthritis. U.S. National Institutes of Health. | ||||
Ref 545653 | 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 525947 | Bioorg Med Chem Lett. 2001 Jan 8;11(1):59-62.Inhibition of RANTES/CCR1-mediated chemotaxis by cosalane and related compounds. | ||||
Ref 529789 | 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 531908 | 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 532913 | Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis. J Med Chem. 2014 Sep 25;57(18):7550-64. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.