Target Information

Target General Infomation
Target ID
T87831
Former ID
TTDR00011
Target Name
FMLP receptor
Gene Name
FPR1
Synonyms
FPR; N-formyl peptide receptor; N-formylpeptide chemoattractant receptor; FPR1
Target Type
Clinical Trial
Disease Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Peptic ulcer [ICD9: 531-534; ICD10: K25-K27]
Function
High affinity receptor for N-formyl-methionyl peptides (fMLP), which are powerful neutrophil chemotactic factors (PubMed:2161213, PubMed:2176894, PubMed:10514456, PubMed:15153520). Binding of fMLP to the receptor stimulates intracellular calcium mobilization and superoxide anion release (PubMed:2161213, PubMed:1712023, PubMed:15153520). This response is mediated via a G-protein that activates a phosphatidylinositol- calcium second messenger system(PubMed:1712023, PubMed:10514456).
BioChemical Class
GPCR rhodopsin
Target Validation
T87831
UniProt ID
P21462
Sequence
METNSSLPTNISGGTPAVSAGYLFLDIITYLVFAVTFVLGVLGNGLVIWVAGFRMTHTVT
TISYLNLAVADFCFTSTLPFFMVRKAMGGHWPFGWFLCKFVFTIVDINLFGSVFLIALIA
LDRCVCVLHPVWTQNHRTVSLAKKVIIGPWVMALLLTLPVIIRVTTVPGKTGTVACTFNF
SPWTNDPKERINVAVAMLTVRGIIRFIIGFSAPMSIVAVSYGLIATKIHKQGLIKSSRPL
RVLSFVAAAFFLCWSPYQVVALIATVRIRELLQGMYKEIGIAVDVTSALAFFNSCLNPML
YVFMGQDFRERLIHALPASLERALTEDSTQTSDTATNSTLPSAEVELQAK
Drugs and Mode of Action
Drug(s) Rebamipide Drug Info Phase 3 Peptic ulcer [525764], [543262]
Antagonist 3570-0208 Drug Info [530431]
BVT173187 Drug Info [531840]
diamide 7 Drug Info [531432]
group E 1682-2106 Drug Info [527699]
methionine benzimidazole 6 Drug Info [531432]
Rebamipide Drug Info [535135]
Agonist AG-09/1 Drug Info [530510]
AG-11/03 Drug Info [531720]
AG-14 Drug Info [528624]
CGEN-855 Drug Info [543577]
compound R-(-)-5f Drug Info [531913]
fMet-Leu-Phe Drug Info [533579]
pyrazolone, 1 Drug Info [532123]
Inhibitor N-formyl-methionyl-leucyl-phenylalanine Drug Info [528815]
Pathways
KEGG Pathway Rap1 signaling pathway
Neuroactive ligand-receptor interaction
Staphylococcus aureus infection
NetPath Pathway Leptin Signaling Pathway
PANTHER Pathway Inflammation mediated by chemokine and cytokine signaling pathway
Pathway Interaction Database Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling
Reactome G alpha (i) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Human Complement System
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 525764The roles of prostaglandin E receptor subtypes in the cytoprotective action of prostaglandin E2 in rat stomach. Aliment Pharmacol Ther. 2000 Apr;14 Suppl 1:116-24.
Ref 543262(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: 871).
Ref 527699Integration of virtual screening with high-throughput flow cytometry to identify novel small molecule formylpeptide receptor antagonists. Mol Pharmacol. 2005 Nov;68(5):1301-10. Epub 2005 Aug 23.
Ref 528624High-throughput screening for small-molecule activators of neutrophils: identification of novel N-formyl peptide receptor agonists. Mol Pharmacol. 2007 Apr;71(4):1061-74. Epub 2007 Jan 17.
Ref 528815Bioorg Med Chem Lett. 2007 Jul 1;17(13):3696-701. Epub 2007 Apr 19.2-Phenyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives: new potent inhibitors of fMLP-induced neutrophil chemotaxis.
Ref 530431Discovery of selective probes and antagonists for G-protein-coupled receptors FPR/FPRL1 and GPR30. Curr Top Med Chem. 2009;9(13):1227-36.
Ref 530510Identification of novel small-molecule agonists for human formyl peptide receptors and pharmacophore models of their recognition. Mol Pharmacol. 2010 Feb;77(2):159-70.
Ref 531432Discovery of small molecule human FPR1 receptor antagonists. Bioorg Med Chem Lett. 2011 May 15;21(10):2991-7.
Ref 531720Molecular docking of 2-(benzimidazol-2-ylthio)-N-phenylacetamide-derived small-molecule agonists of human formyl peptide receptor 1. J Mol Model. 2012 Jun;18(6):2831-43.
Ref 531840A non-peptide receptor inhibitor with selectivity for one of the neutrophil formyl peptide receptors, FPR 1. Biochem Pharmacol. 2012 Jun 15;83(12):1655-62.
Ref 531913Synthesis, enantioresolution, and activity profile of chiral 6-methyl-2,4-disubstituted pyridazin-3(2H)-ones as potent N-formyl peptide receptor agonists. Bioorg Med Chem. 2012 Jun 15;20(12):3781-92.
Ref 532123Functional characterization of three mouse formyl peptide receptors. Mol Pharmacol. 2013 Feb;83(2):389-98.
Ref 533579Further studies on the structural requirements for synthetic peptide chemoattractants. Biochemistry. 1980 May 27;19(11):2404-10.
Ref 535135Rebamipide suppresses formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide production by inhibiting fMLP-receptor binding in human neutrophils. J Pharmacol Exp Ther. 2001 Apr;297(1):388-94.
Ref 543577(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: 222).

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