Target Information
Target General Infomation | |||||
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Target ID |
T97917
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Former ID |
TTDR00540
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Target Name |
FMLP-related receptor I
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Gene Name |
FPR2
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Synonyms |
FMLP-R-I; FPRL1; Formyl peptide receptor-like 1; G-protein-coupled receptor FPR-Like-1; HM63; LXA4 receptor; Lipoxin A4 receptor; RFP; FPR2
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Target Type |
Research
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Function |
Low affinity receptor for N-formyl-methionyl peptides, which are powerful neutrophils chemotactic factors. Binding of FMLP to the receptor causes activation of neutrophils. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system. The activation of LXA4R could result in an anti-inflammatory outcome counteracting the actions of proinflammatory signals such as LTB4 (leukotrieneB4).
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | |||||
Sequence |
METNFSTPLNEYEEVSYESAGYTVLRILPLVVLGVTFVLGVLGNGLVIWVAGFRMTRTVT
TICYLNLALADFSFTATLPFLIVSMAMGEKWPFGWFLCKLIHIVVDINLFGSVFLIGFIA LDRCICVLHPVWAQNHRTVSLAMKVIVGPWILALVLTLPVFLFLTTVTIPNGDTYCTFNF ASWGGTPEERLKVAITMLTARGIIRFVIGFSLPMSIVAICYGLIAAKIHKKGMIKSSRPL RVLTAVVASFFICWFPFQLVALLGTVWLKEMLFYGKYKIIDILVNPTSSLAFFNSCLNPM LYVFVGQDFRERLIHSLPTSLERALSEDSAPTNDTAANSASPPAETELQAM |
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Agonist | AG-26 | Drug Info | [530510] | ||
aspirin triggered lipoxin A4 | Drug Info | [543579] | |||
aspirin-triggered resolvin D1 | Drug Info | [531857] | |||
ATLa2 | Drug Info | [527021] | |||
compound R-(-)-5f | Drug Info | [531913] | |||
fMet-Leu-Phe | Drug Info | [533990] | |||
humanin | Drug Info | [527235] | |||
LXA4 | Drug Info | [530641] | |||
pyrazolone, 1 | Drug Info | [528203] | |||
quin-C1 | Drug Info | [527167] | |||
resolvin D1 | Drug Info | [530641] | |||
RvD1-ME | Drug Info | [531857] | |||
[3H]LXA4 | Drug Info | [526742] | |||
Antagonist | compound 1754-31 | Drug Info | [532404] | ||
quin-C7 | Drug Info | [528957] | |||
Pathways | |||||
Pathway Interaction Database | Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling | ||||
Reactome | G alpha (q) signalling events | ||||
G alpha (i) signalling events | |||||
WikiPathways | GPCRs, Class A Rhodopsin-like | ||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
Peptide GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 526742 | Lipoxin recognition sites. Specific binding of labeled lipoxin A4 with human neutrophils. J Biol Chem. 1992 Aug 15;267(23):16168-76. | ||||
Ref 527021 | Novel 3-oxa lipoxin A4 analogues with enhanced chemical and metabolic stability have anti-inflammatory activity in vivo. J Med Chem. 2004 Apr 8;47(8):2157-65. | ||||
Ref 527167 | A novel nonpeptide ligand for formyl peptide receptor-like 1. Mol Pharmacol. 2004 Nov;66(5):1213-22. Epub 2004 Aug 12. | ||||
Ref 527235 | N-Formylated humanin activates both formyl peptide receptor-like 1 and 2. Biochem Biophys Res Commun. 2004 Nov 5;324(1):255-61. | ||||
Ref 528203 | Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3713-8. Epub 2006 May 11. | ||||
Ref 528957 | Pharmacological characterization of a novel nonpeptide antagonist for formyl peptide receptor-like 1. Mol Pharmacol. 2007 Oct;72(4):976-83. Epub 2007 Jul 25. | ||||
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 530641 | Resolvin D1 binds human phagocytes with evidence for proresolving receptors. Proc Natl Acad Sci U S A. 2010 Jan 26;107(4):1660-5. | ||||
Ref 531857 | Resolvin D1 receptor stereoselectivity and regulation of inflammation and proresolving microRNAs. Am J Pathol. 2012 May;180(5):2018-27. | ||||
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 532404 | Selective agonists and antagonists of formylpeptide receptors: duplex flow cytometry and mixture-based positional scanning libraries. Mol Pharmacol. 2013 Sep;84(3):314-24. |
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