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 | |||||
Sequence |
METNSSLPTNISGGTPAVSAGYLFLDIITYLVFAVTFVLGVLGNGLVIWVAGFRMTHTVT
TISYLNLAVADFCFTSTLPFFMVRKAMGGHWPFGWFLCKFVFTIVDINLFGSVFLIALIA LDRCVCVLHPVWTQNHRTVSLAKKVIIGPWVMALLLTLPVIIRVTTVPGKTGTVACTFNF SPWTNDPKERINVAVAMLTVRGIIRFIIGFSAPMSIVAVSYGLIATKIHKQGLIKSSRPL RVLSFVAAAFFLCWSPYQVVALIATVRIRELLQGMYKEIGIAVDVTSALAFFNSCLNPML YVFMGQDFRERLIHALPASLERALTEDSTQTSDTATNSTLPSAEVELQAK |
||||
Drugs and Mode of Action | |||||
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 527699 | Integration 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 528624 | High-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 528815 | Bioorg 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 530431 | Discovery of selective probes and antagonists for G-protein-coupled receptors FPR/FPRL1 and GPR30. Curr Top Med Chem. 2009;9(13):1227-36. | ||||
Ref 530510 | Identification 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 531432 | Discovery of small molecule human FPR1 receptor antagonists. Bioorg Med Chem Lett. 2011 May 15;21(10):2991-7. | ||||
Ref 531720 | Molecular 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 531840 | A 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 531913 | Synthesis, 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 532123 | Functional characterization of three mouse formyl peptide receptors. Mol Pharmacol. 2013 Feb;83(2):389-98. | ||||
Ref 533579 | Further studies on the structural requirements for synthetic peptide chemoattractants. Biochemistry. 1980 May 27;19(11):2404-10. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.