TABLE 2

Binding affinity and potency of bacterial and mitochondrial formyl peptides pEC50 is defined as the negative logarithm of the EC50. HL-60 cells transfected to express FPR1 or FPR2/ALX, and Chinese hamster ovary cells transfected to express FPR1 were used in some studies

Ligand Origin Assay Potency Cells (Receptors) Reference
N-formyl-Met-Leu-Phe E. coli Chemotaxis pEC50 = 10.15 Neutrophils Showell et al. (1976); Freer et al. (1980)
Lysozyme release pEC50 = 7.49 Neutrophils Freer et al. (1980)
Embedded Image production pEC50 = 7.00 Neutrophils Boxer et al. (1979)
Binding pKd = 9.28–7.61 Neutrophils Koo et al. (1982)
pKd = 6.37 Transfected cells (FPR2/ALX) Quehenberger et al (1993)
N-formyl-Met-Ile-Phe-Leu S. aureus Chemotaxis pEC50 = 7.51 Monocytes Rot et al. (1987)
Competitive binding pIC50 = 8.01 Monocytes Rot et al. (1987)
Embedded Image production pEC50 = 8.00 Neutrophils (mFpr1) Southgate et al. (2008)
N-formyl-Met-Ile-Val-Ile-Leu L. monocytogenes Ca2+ flux pEC50 = 8.66 HL-60 (FPR1) Rabiet et al. (2005)
pEC50 = 6.80 HL-60 (FPR2/ALX) Rabiet et al. (2005)
Embedded Image production pEC50 = 7.82 Neutrophils (mFpr1) Southgate et al. (2008)
N-formyl-Met-Ile-Gly-Trp-Ile L. monocytogenes Ca2+ flux pEC50 = 7.70 HL-60 (FPR1) Rabiet et al. (2005)
pEC50 = 6.68 HL-60 (FPR2/ALX) Rabiet et al. (2005)
N-formyl-Met-Ile-Val-Thr-Leu-Phe L. monocytogenes Ca2+ flux pEC50 = 8.57 HL-60 (FPR1) Rabiet et al. (2005)
pEC50 = 6.70 HL-60 (FPR2/ALX) Rabiet et al. (2005)
N-formyl-Met-Ile-Gly-Trp-Ile-Ile L. monocytogenes Ca2+ flux pEC50 = 7.40 HL-60 (FPR1) Rabiet et al. (2005)
N-formyl-Met-Phy-Glu-Asp-Ala-Val-Ala-Trp-Phy M. avium Chemotaxis pEC50 = 6.00 CHO (FPR1) Gripentrog et al. (2008)
N-formyl-Met-Met-Tyr-Ala-Leu-Phe Mitochondria, ND6 Ca2+ flux pEC50 = 7.92 HL-60 (FPR1) Rabiet et al. (2005)
pEC50 = 7.82 HL-60 (FPR2/ALX) Rabiet et al. (2005)
N-formyl-Met-Leu-Lys-Leu-Ile-Val Mitochondria, ND4 Ca2+ flux pEC50 = 7.92 HL-60 (FPR1) Rabiet et al. (2005)
pEC50 = 7.26 HL-60 (FPR2/ALX) Rabiet et al. (2005)
N-formyl-Met-Tyr-Phe-Ile-Asn-Ile-Leu-Thr-Leu Mitochondria, ND1 Binding pKd = 9.00 CHO (FPR2/ALX) Chiang et al. (2000)
N-formyl-Met-Phe-Ala-Asp-Arg-Trp Cytochrome c oxidase subunit Ca2+ flux pEC50 = 6.80 HL-60 (FPR1) Rabiet et al. (2005)
pEC50 = 6.68 HL-60 (FPR2/ALX) Rabiet et al (2005)
  • CHO, Chinese hamster ovary; pIC50, negative logarithm of the IC50; pEC50, negative logarithm of the EC50