Table 1.

Structures and sequences of representative FPR ligands. The table shows selected FPR ligands in different categories, based on their origins and chemical structures. Ac = acetyl; Me = methyl; Ph = phenyl; Pam = palmitoyl; N.D, binding affinity or potency not determined.

Ligands Representatives	Sequence/Structure	Selectivity	Reference
Agonists
N-Formyl peptides
a. Bacteria-derived formyl peptides
fMLF	formyl-Met-Leu-Phe	FPR1 > FPR2	[40]
PSMα peptide	formyl-MGIIAGIIKFI KGLIEKFTGK	FPR2 > FPR1	[52]
b. Mitochondria-derived formyl peptides
fMMYALF	formyl-Met-Met-Tyr-Ala-Leu-Phe	FPR1, FPR2	[53]
Mitocryptide-2	formyl-MTNIRKSHPLMKIIN	FPR2	[54]
Non-formyl peptides
a. Microbe-derived peptides
Hp2-20	AKKVFKRLEKLFSKIQNDK	FPR2 >> FPR3	[55]
b. Host-derived peptides
SAA1.1		FPR2, others	[56,57]
Aβ42	DAEFRHDSGYEVHHQKLVFFAEDVGSNKGAIIGLMVGGVVIA	FPR2	[28,58]
Ac2–26	Ac-AMVSEFLKQAWFIENEEQEYVQTVK	FPR1, FPR2	[59,60]
LL-37	LLGDFFRKSKEKIGKEFKRIVQRIKDFLRNLVPRTES	FPR2	[61]
uPAR88-92	88Ser-Arg-Ser-Arg-Tyr92 (SRSRY)	FPR1	[62]
uPAR84-95	AVTYSRSRYLEC	FPR2, FPR3	[63]
PrP(106-126)	KTNMKHMAGAAAAGAVVGGLG	FPR2	[64]
SHAAGtide	MLWRRKIGPQMTLSHAAG	FPR2 > CCR1	[65]
VIP	HSDAVFTDNYTRLRKQMAVKKYLNSILN	FPR2, VPAC1	[66]
c. Synthetic peptides
W peptides	WKYMVm(Trp-Lys-Tyr-Met-Val-D-Met-NH2)	FPR2 > FPR1 >> FPR3	[67,68,69]
	WKYMVM(Trp-Lys-Tyr-Met-Val-Met-NH2)	FPR2 >> FPR3	[69]
MMK1	LESIFRSLLFRVM	FPR2	[70]
L-37pA	DWLKAFYDKVAEKLKEAFPDWLKAFYDKVAEKLKEAF	FPR2	[71]
CGEN-855A	TIPMFVPESTSKLQKFTSWFM	FPR2, FPR3	[72]
d. Pepducins
F2Pal16	Pam-KIHKKGMIKSSRPLRV	FPR2	[72,73]
Eicosanoids
Lipoxin A4			[74]
Small molecules
a. Quinazolinones Quin-C1		FPR2 >> FPR1	[75]
b. Benzimidazoles AG-09/1		FPR1	[76]
c. N-substituted benzimidazole derivative N-substituted benzimidazole 11		FPR2	[77]
d. Pyrazolones Compound 43		FPR2 > FPR1	[78,79]
e. Pyridazin-3(2H)-ones Pyridazin-3(2H)-one derivative 1		FPR1	[80]
Pyridazin-3(2H)-one derivative 2		FPR2	[80]
f. N-phenylureas AG-26		FPR2	[76]
g. Chiral pyridazines	R = n-C3H7, i-C3H7, n-C4H9	FPR1, FPR2	[81]
h. 2-(N-Piperazinyl) acetamide derivatives AG-09/73		FPR2	[76]
i. chiral 3-(1H-indol-3-yl)-2-[3-(4-nitrophenyl)ureido]propanamides PD176252		FPR2	[82,83]
j. Others 1753-103		FPR1	[84]
Antagonists
Peptides
a. Natural peptides & analogs
Boc-1	N-tert-butoxycarbonyl-MLF	FPR1 >> FPR2	[40]
Boc-2	N-tert-butoxycarbonyl-FLFLF	FPR1 >> FPR2	[40]
CHIP peptide     Uteroglobin (UG)	FTFEPF MKLAVTLTLVTLALCCSSASAEICPSFQRVIETLLMDTPSSYEAAMELFSPDQDMREAGAQLKKLVDTLPQKPRESIIKLMEKIAQSSLCN	FPR1 FPR2	[85] [86]
Cyclosporin H (CsH)		FPR1	[87]
Cyclized uPAR88-92	[88Ser-Arg-Ser-Arg-Tyr92]( cyclized SRSRY)	FPR1, N.D for FPR2	[88]
b. Synthetic peptides
WRW4	WRWWWW (Trp-Arg-Trp-Trp-Trp-Trp)	FPR2, FPR3	[89]
PBP10	RhoB-QRLFQVKGRR	FPR2, others	[90]
Lipopeptides
F1Pal16	Pam-KIHKQGMIKSSRPLRV	FPR2	[91]
Pam-(Lys-βNSpe)6-NH2		FPR2, mFpr2	[92,93]
Non-peptide molecules
Isoflavone analog		FPR1	[94]
1754-31		FPR2	[84]
Quin-C7		FPR2	[95]