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Synonyms: Trp-Lys-Tyr-Met-Val-[D]Met | WKYMVM
Compound class:
Peptide
Comment: Peptide agonist of FPR1, FPR2 and FPR3 receptors.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| References |
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1. Bozinovski S, Anthony D, Anderson GP, Irving LB, Levy BD, Vlahos R. (2013)
Treating neutrophilic inflammation in COPD by targeting ALX/FPR2 resolution pathways. Pharmacol Ther, 140 (3): 280-9. [PMID:23880288] |
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2. Christophe T, Karlsson A, Dugave C, Rabiet MJ, Boulay F, Dahlgren C. (2001)
The synthetic peptide Trp-Lys-Tyr-Met-Val-Met-NH2 specifically activates neutrophils through FPRL1/lipoxin A4 receptors and is an agonist for the orphan monocyte-expressed chemoattractant receptor FPRL2. J Biol Chem, 276 (24): 21585-93. [PMID:11285256] |
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3. Clish CB, O'Brien JA, Gronert K, Stahl GL, Petasis NA, Serhan CN. (1999)
Local and systemic delivery of a stable aspirin-triggered lipoxin prevents neutrophil recruitment in vivo. Proc Natl Acad Sci USA, 96 (14): 8247-52. [PMID:10393980] |
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4. Fiore S, Maddox JF, Perez HD, Serhan CN. (1994)
Identification of a human cDNA encoding a functional high affinity lipoxin A4 receptor. J Exp Med, 180 (1): 253-60. [PMID:8006586] |
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5. Fiore S, Serhan CN. (1995)
Lipoxin A4 receptor activation is distinct from that of the formyl peptide receptor in myeloid cells: inhibition of CD11/18 expression by lipoxin A4-lipoxin A4 receptor interaction. Biochemistry, 34 (51): 16678-86. [PMID:8527441] |
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6. Gabl M, Sundqvist M, Holdfeldt A, Lind S, Mårtensson J, Christenson K, Marutani T, Dahlgren C, Mukai H, Forsman H. (2018)
Mitocryptides from Human Mitochondrial DNA-Encoded Proteins Activate Neutrophil Formyl Peptide Receptors: Receptor Preference and Signaling Properties. J Immunol, 200 (9): 3269-3282. [PMID:29602776] |
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7. García RA, Lupisella JA, Ito BR, Hsu MY, Fernando G, Carson NL, Allocco JJ, Ryan CS, Zhang R, Wang Z et al.. (2021)
Selective FPR2 Agonism Promotes a Proresolution Macrophage Phenotype and Improves Cardiac Structure-Function Post Myocardial Infarction. JACC Basic Transl Sci, 6 (8): 676-689. [PMID:34466754] |
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8. Gronert K, Martinsson-Niskanen T, Ravasi S, Chiang N, Serhan CN. (2001)
Selectivity of recombinant human leukotriene D(4), leukotriene B(4), and lipoxin A(4) receptors with aspirin-triggered 15-epi-LXA(4) and regulation of vascular and inflammatory responses. Am J Pathol, 158 (1): 3-9. [PMID:11141472] |
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9. He HQ, Liao D, Wang ZG, Wang ZL, Zhou HC, Wang MW, Ye RD. (2013)
Functional characterization of three mouse formyl peptide receptors. Mol Pharmacol, 83 (2): 389-98. [PMID:23160941] |
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10. He R, Tan L, Browning DD, Wang JM, Ye RD. (2000)
The synthetic peptide Trp-Lys-Tyr-Met-Val-D-Met is a potent chemotactic agonist for mouse formyl peptide receptor. J Immunol, 165 (8): 4598-605. [PMID:11035102] |
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11. Le Y, Gong W, Li B, Dunlop NM, Shen W, Su SB, Ye RD, Wang JM. (1999)
Utilization of two seven-transmembrane, G protein-coupled receptors, formyl peptide receptor-like 1 and formyl peptide receptor, by the synthetic hexapeptide WKYMVm for human phagocyte activation. J Immunol, 163 (12): 6777-84. [PMID:10586077] |
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12. Lin H, Ma C, Cai K, Guo L, Wang X, Lv L, Zhang C, Lin J, Zhang D, Ye C et al.. (2025)
Metabolic signaling of ceramides through the FPR2 receptor inhibits adipocyte thermogenesis. Science, 388 (6746): eado4188. [PMID:40080544] |
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13. Peng C, Vecchio EA, Nguyen ATN, De Seram M, Tang R, Keov P, Woodman OL, Chen YC, Baell J, May LT et al.. (2024)
Biased receptor signalling and intracellular trafficking profiles of structurally distinct formylpeptide receptor 2 agonists. Br J Pharmacol, 181 (22): 4677-4692. [PMID:39154373] |
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14. Perretti M, Flower RJ. (1995)
Anti-inflammatory lipocortin-derived peptides. Agents Actions Suppl, 46: 131-8. [PMID:7610983] |
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15. Qin CX, May LT, Li R, Cao N, Rosli S, Deo M, Alexander AE, Horlock D, Bourke JE, Yang YH et al.. (2017)
Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice. Nat Commun, 8: 14232. [PMID:28169296] |
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16. Rabiet MJ, Huet E, Boulay F. (2005)
Human mitochondria-derived N-formylated peptides are novel agonists equally active on FPR and FPRL1, while Listeria monocytogenes-derived peptides preferentially activate FPR. Eur J Immunol, 35 (8): 2486-95. [PMID:16025565] |
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17. Takano T, Fiore S, Maddox JF, Brady HR, Petasis NA, Serhan CN. (1997)
Aspirin-triggered 15-epi-lipoxin A4 (LXA4) and LXA4 stable analogues are potent inhibitors of acute inflammation: evidence for anti-inflammatory receptors. J Exp Med, 185 (9): 1693-704. [PMID:9151906] |
