Agonists for the human FPRs The agonists are listed in the order of their potency within each group. The mitochondrial N-formylated peptides, listed in the first group, are also host-derived peptides. A more detailed list of N-formyl peptides is given in Table 2. Ligands that have been isolated from living organisms in the forms listed, and those generated by the actions of physiologically relevant enzymes, are indicated with an asterisk (*)
| Ligand | Origin/Description | Potency | Selectivity | Reference |
|---|---|---|---|---|
| N-formyl peptides | ||||
| fMLF and other bacterial formyl peptides* | Bacteria | (see Table 2) | FPR1 > FPR2/ALX | (see Table 2) |
| Mitochondrial formyl peptides* | Mitochondria | (see Table 2) | FPR1 ≈ FPR2/ALX | (see Table 2) |
| N-formyl-Nle-Leu-Phe-Nle-Tyr-Lys | Synthetic | pKd = 9.22 | FPR1 ≫ FPR2/ALX | Sklar et al. (1984) |
| Microbe-derived nonformyl peptides | ||||
| T20 (DP178) | HIV-1 gp41 aa. 643–678 | pEC50 = 8.30 | FPR1 | Su et al. (1999c) |
| Hp (2–20) | H. pylori | pEC50 = 6.52 | FPR2/ALX ≫ FPR3 | Betten et al. (2001) |
| T21 (DP107) | HIV-1 gp41 aa. 558–595 | pEC50 = 6.30 | FPR2/ALX | Su et al. (1999a) |
| V3 peptide | HIV-1 gp120, V3 loop | pEC50 = 5.82 | FPR2/ALX | Shen et al. (2000) |
| N36 peptide | HIV-1 gp41 aa. 546–581 | pEC50 = 5.00 | FPR2/ALX | Le et al. (2000b) |
| F peptide | HIV-1 gp120 aa. 414–434 | pEC50 = 5.00 | FPR2/ALX | Deng et al. (1999) |
| Host-derived peptides | ||||
| CKβ8–1 (human CCL23)* | Chemokine | pEC50 = 9.00–7.82 | FPR2/ALX ≈ CCR1 | Elagoz et al. (2004) |
| SHAAGtide* | CCL23 N-terminal 18 aa. | pEC50 = 7.72 | FPR2/ALX > CCR1 | Miao et al. (2007) |
| Humanin* | Neuroprotective peptide | pEC50 = 8.46 | FPR2/ALX | Harada et al. (2004); Ying et al. (2004) |
| F2L* | Heme binding protein | pEC50 = 8.00 | FPR3 ≫ FPR2/ALX | Migeotte et al. (2005) |
| SAA* | Acute-phase protein | pEC50 = 7.35 | FPR2/ALX, others | Su et al. (1999b) |
| Annexin 1 / lipocortin 1* | pIC50 = 6.82 | FPR1 | Walther et al. (2000) | |
| Ac2–26* | Annexin 1 | pEC50 = 6.05–5.77 | FPR1, FPR2/ALX | Perretti et al. (2002); Hayhoe et al. (2006) |
| Ac9–25 | Annexin 1 | pEC50 = 4.70 | FPR1, FPR2/ALX | Karlsson et al. (2005) |
| Aβ (1–42)* | Amyloid precursor | pEC50 = 7.00 | FPR2/ALX | Le et al. (2001a); Tiffany et al. (2001) |
| D2D3* | uPAR (88–274) | pEC50 = 7.08 | FPR2/ALX | Resnati et al. (2002) |
| LL-37* | Cathelicidin | pEC50 = 6.00 | FPR2/ALX | Yang et al. (2000) |
| PrP (106–126)* | Prion protein | pEC50 = 4.60 | FPR2/ALX | Le et al. (2001b) |
| Temporin (from Rana temporaria)* | Anti-microbial peptide | pEC50 = 6.60 | FPR2/ALX | Chen et al. (2004) |
| Pituitary adenylate cyclase activating polypeptide | pEC50 = 6.00 | FPR2/ALX | Kim et al. (2006) | |
| Host-derived nonpeptide agonists | ||||
| Lipoxin A4 and aspirin-triggered lipoxins* | Eicosanoids | pKd = 8.77 | FPR2/ALX, AhR | Fiore et al. (1994) |
| Agonists from peptide library | ||||
| WKYMVm | Peptide library | pEC50 = 10.13 | FPR2/ALX > FPR ≫ FPR3 | Le et al. (1999); Christophe et al. (2001) |
| WKYMVM | Peptide library | pEC50 = 8.70 | FPR2/ALX ≫ FPR3 | Christophe et al. (2001) |
| MMK-1 | Peptide library | pEC50 = 8.70 | FPR2/ALX | Klein et al. (1998); Hu et al. (2001) |
| MMWLL, formyl-MMWLL | Peptide library | pEC50 = 8.96 | FPR1 | Chen et al. (1995) |
| Agonists from nonpeptide library | ||||
| Quinazolinone derivative (Quin-C1) | Combinatorial library | pEC50 = 5.72 | FPR2/ALX ≫ FPR1 | Nanamori et al. (2004) |
| Pyrazolone, 4-iodo-substituted, no. 43 | Combinatorial library | pIC50 = 7.36 | FPR2/ALX ≫ FPR1 | Bürli et al. (2006) |
| AG-14 | Drug-like molecule library | pEC50 = 7.38 | FPR1 | Schepetkin et al. (2007) |
aa., amino acid; pIC50, negative logarithm of the IC50; pEC50, negative logarithm of the EC50; pKd, negative logarithm of Kd