Target Information

Target General Infomation
Target ID
T15439
Former ID
TTDNC00518
Target Name
C5aR
Gene Name
C5AR1
Synonyms
C5a anaphylatoxin chemotactic receptor; C5a anaphylatoxin chemotactic receptor 1; CD88; C5AR1
Target Type
Clinical Trial
Disease Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Vasculitis [ICD10: I77.6, I80]
Function
Receptor for the chemotactic and inflammatory peptideanaphylatoxin C5a (PubMed:1847994, PubMed:8182049, PubMed:7622471, PubMed:9553099, PubMed:10636859, PubMed:15153520). The ligand interacts with at least two sites on the receptor: a high-affinity site on the extracellular N-terminus, and a second site in the transmembrane region which activates downstream signaling events (PubMed:8182049, PubMed:7622471, PubMed:9553099). Receptor activation stimulates chemotaxis, granule enzyme release, intracellular calcium release and superoxide anion production (PubMed:10636859, PubMed:15153520).
BioChemical Class
GPCR rhodopsin
UniProt ID
P21730
Sequence
MDSFNYTTPDYGHYDDKDTLDLNTPVDKTSNTLRVPDILALVIFAVVFLVGVLGNALVVW
VTAFEAKRTINAIWFLNLAVADFLSCLALPILFTSIVQHHHWPFGGAACSILPSLILLNM
YASILLLATISADRFLLVFKPIWCQNFRGAGLAWIACAVAWGLALLLTIPSFLYRVVREE
YFPPKVLCGVDYSHDKRRERAVAIVRLVLGFLWPLLTLTICYTFILLRTWSRRATRSTKT
LKVVVAVVASFFIFWLPYQVTGIMMSFLEPSSPTFLLLKKLDSLCVSFAYINCCINPIIY
VVAGQGFQGRLRKSLPSLLRNVLTEESVVRESKSFTRSTVDTMAQKTQAV
Drugs and Mode of Action
Drug(s) CCX-168 Drug Info Phase 2 Vasculitis [525112]
PMX-53 Drug Info Phase 2 Atopic dermatitis [531408], [541109]
NN8209 Drug Info Discontinued in Phase 2 Rheumatoid arthritis [548112]
NN8210 Drug Info Discontinued in Phase 1 Rheumatoid arthritis [549391]
Modulator C5aR pepducins Drug Info [543765]
NN8209 Drug Info [532298]
NN8210 Drug Info [532298]
PMX-53 Drug Info
Antagonist CCX-168 Drug Info [550548]
NDT9520492 Drug Info [527806]
RPR121154 Drug Info [543765]
W54011 Drug Info [526441]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Complement and coagulation cascades
Staphylococcus aureus infection
PANTHER Pathway Inflammation mediated by chemokine and cytokine signaling pathway
Reactome Peptide ligand-binding receptors
G alpha (i) signalling events
WikiPathways Complement and Coagulation Cascades
Human Complement System
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 525112ClinicalTrials.gov (NCT02384317) Open-Label Study to Evaluate Safety and Efficacy of CCX168 in Subjects With Immunoglobulin A Nephropathy on Stable RAAS Blockade. U.S. National Institutes of Health.
Ref 531408PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol Pharmacol. 2011 Jun;79(6):1005-13.
Ref 541109(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: 579).
Ref 548112Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022053)
Ref 549391Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036376)
Ref 526441Identification of a potent and orally active non-peptide C5a receptor antagonist. J Biol Chem. 2002 Dec 20;277(51):49403-7. Epub 2002 Oct 15.
Ref 527806Molecular characterization of the gerbil C5a receptor and identification of a transmembrane domain V amino acid that is crucial for small molecule antagonist interaction. J Biol Chem. 2005 Dec 9;280(49):40617-23. Epub 2005 Oct 17.
Ref 532298Complement in immune and inflammatory disorders: therapeutic interventions. J Immunol. 2013 Apr 15;190(8):3839-47.
Ref 543765(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: 32).
Ref 550548Clinical pipeline report, company report or official report of ChemoCentryx.

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