Page last updated: 2024-12-05

n-formylmethionine leucyl-phenylalanine

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Description

N-Formylmethionine Leucyl-Phenylalanine: A formylated tripeptide originally isolated from bacterial filtrates that is positively chemotactic to polymorphonuclear leucocytes, and causes them to release lysosomal enzymes and become metabolically activated. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

N-formyl-L-methionyl-L-leucyl-L-phenylalanine : A tripeptide composed of L-Met, L-Leu and L-Phe in a linear sequence with a formyl group at the amino terminus. It acts as a potent inducer of leucocyte chemotaxis and macrophage activator as well as a ligand for the FPR receptor. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID443295
CHEMBL ID267179
CHEBI ID53490
SCHEMBL ID39529
MeSH IDM0014396

Synonyms (50)

Synonym
MLS002207097
n-formylmethionine-leucine-phenylalanine
bdbm50050937
(s)-2-[(s)-2-((s)-2-formylamino-4-methylsulfanyl-butyrylamino)-4-methyl-pentanoylamino]-3-phenyl-propionic acid
gtpl1022
formyl-met-leu-phe
MLS001361389
n-formyl-met-leu-phe
smr000857394
fmlp
n-formyl-l-methionyl-l-leucyl-l-phenylalanine
59880-97-6
formyl met leu phe
n-formyl-met-leu-phe, >=97% (hplc)
f-met-leu-phe
n-formyl-methionyl-leucyl-phenylalanine
fmlf
fmet-leu-phe
n-formylmethionine leucyl-phenylalanine
n-formyl-met-leu-phe, bioxtra, >=99.0% (tlc)
CHEMBL267179 ,
(2s)-2-[[(2s)-2-[[(2s)-2-formamido-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoic acid
CHEBI:53490 ,
fmetleuphe
HMS2235B23
chemotactic peptide
SCHEMBL39529
AKOS024456858
mfcd00036780
DTXSID9041077
chemotactic peptide (for-l-met-l-leu-l-phe-oh)
CS-6489
HY-P0224
(s)-2-((s)-2-((s)-2-formamido-4-(methylthio)butanamido)-4-methylpentanamido)-3-phenylpropanoic acid
l-phenylalanine, n-formyl-l-methionyl-l-leucyl-
AS-57764
(2s)-2-[(2s)-2-[(2s)-2-formamido-4-(methylsulfanyl)butanamido]-4-methylpentanamido]-3-phenylpropanoic acid
Q5090627
formyl-met-leu-phe-oh - cas 59880-97-6
(2s)-2-(((2s)-2-(((2s)-2-formamido-4-methylsulfanylbutanoyl)amino)-4-methylpentanoyl)amino)-3-phenylpropanoic acid
n-(n-(n-formyl-l-methionyl)-l-leucyl)
f-met-leu-phe l-phenylalanine
PRQROPMIIGLWRP-BZSNNMDCSA-N
formyl-methionyl-leucyl-phenylalanine
n-formyl-mlf
D90695
fmlp; n-formyl-mlf
GLXC-26059
(s)-2-((s)-2-((s)-2-formamido-4-(methylthio)butanamido)-4-methylpentanamido)-3-phenylpropanoicacid
F1158

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" In addition, time to maximal activity and half-life differed in PMNs and in plasma (4."( Pharmacokinetics and pharmacodynamics of neutrophil-associated ciprofloxacin in humans.
Blardi, P; Capecchi, PL; Ceccatelli, L; De Lalla, A; Di Perri, T; Pasini, L; Volpi, L, 1995
)
0.29
" Pharmacokinetic studies indicate that after oral dosing L-680,833 is bioavailable in rats and rhesus monkeys."( Chemical, biochemical, pharmacokinetic, and biological properties of L-680,833: a potent, orally active monocyclic beta-lactam inhibitor of human polymorphonuclear leukocyte elastase.
Brause, K; Chandler, GO; Doherty, JB; Dorn, CP; Finke, PE; Hagmann, WK; Hale, JJ; Kissinger, AL; Shah, SK; Thompson, KR, 1993
)
0.29
" This method has utility in evaluating the pharmacodynamic action of either LTB(4) receptor antagonists or immune cell modulators in effecting CD11b integrin expression and granulocyte activation in human subjects administered such drugs."( Human granulocyte CD11b expression as a pharmacodynamic biomarker of inflammation.
Carpenter, DC; Davis, HM; Griswold, DE; Hynicka, WP; Stahl, JM; Zhang, W, 2000
)
0.31
" Pharmacokinetic properties and tissue distribution also differed between nanocarriers with and without fMLF."( Peritoneal macrophage uptake, pharmacokinetics and biodistribution of macrophage-targeted PEG-fMLF (N-formyl-methionyl-leucyl-phenylalanine) nanocarriers for improving HIV drug delivery.
Hu, P; Leibowitz, MJ; Pooyan, S; Sinko, PJ; Stein, S; Wan, L, 2007
)
0.34

Bioavailability

ExcerptReferenceRelevance
" This oral bioavailability is reflected by the inhibition (i) of tissue damage elicited in hamster lungs by intratracheal instillation of human PMNE and (ii) enzyme released from human PMN stimulated after their transfer into the pleural cavity of mice."( Chemical, biochemical, pharmacokinetic, and biological properties of L-680,833: a potent, orally active monocyclic beta-lactam inhibitor of human polymorphonuclear leukocyte elastase.
Brause, K; Chandler, GO; Doherty, JB; Dorn, CP; Finke, PE; Hagmann, WK; Hale, JJ; Kissinger, AL; Shah, SK; Thompson, KR, 1993
)
0.29
" The administration of Cu(II), whether complexed with linear oligopeptides or as an inorganic salt, to animals or tissue extracts, conferred protection against oxidation and ought, conceivably, to interact with endogenous biological molecules and form highly bioavailable complexes which serve, subsequently, as the real scavengers."( An in vivo, ex vivo and in vitro comparative study of activity of copper oligopeptide complexes vs Cu(II) ions.
Cellai, C; Chelli, M; Ciuffi, M; Franchi-Micheli, S; Ginanneschi, M; Paoletti, F; Papini, AM; Zilletti, L, 1998
)
0.3
" Thus to further improve the NAC bioavailability a single oral administration of 1200 mg NAC has been recently proposed."( Human neutrophil oxidative bursts and their in vitro modulation by different N-acetylcysteine concentrations.
Allegra, L; Bovio, C; Braga, PC; Dal Sasso, M; Fonti, E; Massoni, C, 2002
)
0.31
" Pharmacokinetic data in the rat demonstrated approximately 100% bioavailability of the agent."( Pharmacological profile of CR3465, a new leukotriene CysLT1 receptor antagonist with broad anti-inflammatory activity.
Caselli, G; Ferrari, F; Makovec, F; Mennuni, L; Zanelli, T, 2004
)
0.32

Dosage Studied

ExcerptRelevanceReference
" The dose-response curves for NKA and SP were shifted to the left (three orders and one order of magnitude, respectively) in AMs isolated from sensitized animals, with no variation in maximal effects."( Enhanced responsiveness of ovalbumin-sensitized guinea-pig alveolar macrophages to tachykinins.
Brunelleschi, S; Ceni, E; Fantozzi, R; Giotti, A; Parenti, A, 1992
)
0.28
" Based on dose-response experiments, the relative rank order of potency for the three chemoattractants was: LTB4 = FMLP greater than PAF for filter alone barrier; LTB4 greater than FMLP greater than PAF for HUVE cell barrier; and FMLP greater than LTB4 greater than PAF for MDCK and A549 epithelial cell barriers."( Degree of neutrophil chemotaxis is dependent upon the chemoattractant and barrier.
Abbas, MK; Carolan, EJ; Casale, TB, 1992
)
0.28
" Evaluation of chemotaxis demonstrated that cord blood neutrophils exhibited a shift in the fMLP dose-response relationship showing relatively better chemotaxis to lower concentrations."( Effect of low neutral endopeptidase expression on response to fMLP.
Basford, RE; Kaplan, SS; Park, J; Penchansky, L; Zdziarski, UE, 1992
)
0.28
" Dose-response studies performed on blood from normal healthy volunteers showed higher maximal secretory responses in males than females (33."( Assessment of neutrophil leukocyte secretory response to fMLP in whole blood in vitro.
Butt, TJ; Chadwick, VS; Ferry, DM, 1992
)
0.28
" In the presence of LDLLFL, the FMLP dose-response curve shifted to higher concentrations, indicating that LDLLFL interfered with binding of FMLP to its receptor."( An immunosuppressive retrovirus-derived hexapeptide interferes with intracellular signaling in monocytes and granulocytes through N-formylpeptide receptors.
Knol, EF; Oostendorp, RA; Scheper, RJ; Verhoeven, AJ, 1992
)
0.28
" The dose-response to f-Met-Leu-Phe in TNF-primed cells demonstrated the same half-maximal and maximal concentrations of f-Met-Leu-Phe as seen in untreated cells."( Priming of the HL-60 cell respiratory burst response by tumor necrosis factor-alpha.
Klein, JB; McLeish, KR; Sonnenfeld, G, 1991
)
0.28
" Oral dosing of nilvadipine suppressed carrageenan-induced paw edema (ED30:15 mg/kg in rats and 20 mg/kg in mice) at a potency corresponding to that of an anti-inflammatory drug, ibuprofen."( Inhibition by nilvadipine of ischemic and carrageenan paw edema as well as of superoxide radical production from neutrophils and xanthine oxidase.
Oyanagui, Y; Sato, S, 1991
)
0.28
" Administration of erythromycin to asthmatic patients in a dosage of 600 mg/d for 10 weeks reduced the bronchial hyperresponsiveness measured by histamine inhalation test."( Effect of erythromycin on bronchial hyperresponsiveness in patients with bronchial asthma.
Miyatake, H; Satake, T; Suzuki, K; Takagi, K; Taki, F, 1991
)
0.28
" Passive sensitization with IgE-rich plasma caused a significant increase in maximal anti-IgE-induced HR in the majority of cord blood samples, and the dose-response curve was similar to that obtained in adult blood."( Comparison of histamine release in cord blood and adult blood.
Bjerke, T; Engberg, TM; Nielsen, BW; Schiøtz, PO, 1991
)
0.28
" The dose-response curves for priming were identical to those for triggering of an increase in [Ca2+]i and pHi."( Stimulation and priming of human neutrophils by interleukin-8: cooperation with tumor necrosis factor and colony-stimulating factors.
Kasahara, T; Kitagawa, S; Matsushima, K; Saito, M; Takaku, F; Yuo, A, 1991
)
0.28
" However, after an FMLP dose-response curve in rabbits, tachyphylaxis to a second challenge was seen in some rabbits and airway inflammation was absent."( Effects of prolonged inhalation of N-formyl-methionyl-leucyl-phenylalanine in rabbits.
Berend, N; Breslin, AB; Panaretto, K; Peters, MJ, 1991
)
0.28
" The dose-response dependence of the effect (10(-15)-10(-9) M) followed a characteristic biphasic pattern (with the maximum effect at ultra-low doses)."( Respiratory burst inhibition in human neutrophils by ultra-low doses of [D-Ala2]methionine enkephalinamide.
Koshkin, AA; Sazanov, LA; Sud'ina, GF; Varfolomeev, SD; Zaitsev, SV, 1991
)
0.28
" The dose-response curve for FMLP was biphasic; low concentrations were stimulatory, and the response was reduced at higher concentrations."( The involvement of calcium and protein kinase C in modulating agonist-stimulated chemotaxis of human neutrophils.
Greener, M; Hallam, TJ; Merritt, JE; Swayne, GT, 1991
)
0.28
" Dose-response experiments revealed a K0."( Functional reconstitution of fMet-Leu-Phe receptor in Xenopus laevis oocytes.
Coats, WD; Navarro, J, 1990
)
0.28
" The similarity of the dose-response curves for superoxide production and lysozyme secretion indicates that the early transmembrane signalling events are identical for the two responses studied."( Polymeric analogues of N-formyl peptides are potent activators of degranulation and superoxide production by human neutrophils.
Kraus, JL; Lederer, F; Ravel, P, 1990
)
0.28
"0 microM f-Met peptide), although anti-IgE-induced release was unaffected over a dose-response curve."( The effect of pertussis toxin on mediator release from human basophils.
MacGlashan, DW; Warner, JA; Yancey, KB, 1987
)
0.27
"The influence of major histocompatibility complex (B complex) dosage on monocyte-macrophage function was examined using 4- to 6-week-old trisomic strain chickens."( Effects of increased major histocompatibility complex dosage on chicken monocyte-macrophage function.
Bloom, SE; Dietert, RR; Qureshi, MA, 1989
)
0.28
" NAF showed activity over a wider concentration range and its dose-response curve was less steep than that of the two other agonists."( Histamine and sulfidoleukotriene release from human basophils: different effects of antigen, anti-IgE, C5a, f-Met-Leu-Phe and the novel neutrophil-activating peptide NAF.
Baggiolini, M; Dahinden, CA; Dewald, B; Kurimoto, J; Walz, A, 1989
)
0.28
" Based on a comparison of dose-response curves for inhibition of fluoresceinated fMet-Leu-Phe-Lys binding, the relative affinity of the peptide for the receptor was comparable to that of fMet-Leu-Phe-Lys."( Staphylococcus aureus tetrapeptide with high chemotactic potency and efficacy for human leukocytes.
Henderson, LE; Leonard, EJ; Rot, A; Sowder, R, 1989
)
0.28
" Ten non-asthmatic subjects aged 21-28 yrs performed dose-response curves to nebulized FMLP on 3 study days after pretreatment with saline, F or IB."( The effect of anticholinergic and beta-agonist pretreatment on bronchoconstriction induced by N-formyl-methionyl-leucyl-phenylalanine.
Berend, N; Breslin, AB; Peters, MJ, 1989
)
0.28
" The dose-response relationship for fMLP-induced LDCL of neutrophils preincubated with rhGM-CSF revealed that half-maximum enhancement was achieved at an approximately 20-fold higher concentration than that of colony-forming units in culture-derived colony formation."( Effect of granulocyte-macrophage colony-stimulating factor on chemiluminescence of human neutrophils.
Niho, Y; Okamura, S; Otsuka, T; Yamaga, S, 1989
)
0.28
" The dose-response curves for triggering of O2- release and membrane depolarization by each of receptor-mediated agonists in phorbol myristate acetate-pretreated or control cells were identical."( Phorbol myristate acetate potentiates superoxide release and membrane depolarization without affecting an increase in cytoplasmic free calcium in human granulocytes stimulated by the chemotactic peptide, lectins and the calcium ionophore.
Kitagawa, S; Miura, Y; Ohsaka, A; Saito, M; Suzuki, I; Takaku, F, 1988
)
0.27
" On a separate day the FMLP dose-response curves were repeated after nebulisation of 500 micrograms of ipratropium bromide."( Effect of inhaled formyl-methionyl-leucyl-phenylalanine on airway function.
Armour, CL; Berend, N; Black, JL; Peters, MJ; Ward, HE, 1988
)
0.27
" The mechanism of deactivation of PAM does not appear to result from a shift in the dose-response curve or decreased availability of membrane receptors, but may involve uncoupling of post-receptor cellular responses."( Deactivation of guinea pig pulmonary alveolar macrophage responses to N-formyl-methionyl-leucyl-phenylalanine: chemotaxis, superoxide generation, and binding.
Atkinson, JP; Daughaday, CC; Mehta, J; Spilberg, I, 1985
)
0.27
" Incubation of the neutrophils with cholera toxin, unlike pertussis toxin, did not inhibit the fMet-Leu-Phe induced rise in the intracellular concentration of free calcium, and caused only a shift to the right of the dose-response curve of N-acetyl-beta-glucosaminidase release."( Pertussis but not cholera toxin inhibits the stimulated increase in actin association with the cytoskeleton in rabbit neutrophils: role of the "G proteins" in stimulus-response coupling.
Becker, EL; Feinstein, MB; Molski, TF; Munoz, JJ; Naccache, PH; Sha'afi, RI; Shefcyk, J; Volpi, M; Yassin, R, 1985
)
0.27
" The leukotriene-generating response of monolayers of human monocytes pretreated with cytochalasin B to FMLP is receptor-mediated, as indicated by the inactivity of the structural analog N-acetyl-methionyl-leucyl-phenylalanine and by the capacity of the FMLP receptor antagonist carbobenzoxyphenylalanyl-methionine to inhibit the agonist action of FMLP in a dose-response fashion."( Generation of leukotrienes by human monocytes pretreated with cytochalasin B and stimulated with formyl-methionyl-leucyl-phenylalanine.
Austen, KF; Lee, TH; Lewis, RA; Robin, JL; Williams, JD, 1986
)
0.27
" Dose-response studies indicated that phosphorylation of the 67 kilodalton protein was particularly sensitive to inhibition by quercetin at concentrations that also inhibit neutrophil degranulation and superoxide production."( The bioflavonoid quercetin inhibits neutrophil degranulation, superoxide production, and the phosphorylation of specific neutrophil proteins.
Blackburn, WD; Heck, LW; Wallace, RW, 1987
)
0.27
" Dose-response curves indicated variations in the sensitivity of monocytes and granulocytes to these mediators."( Stimulated mobilization of monocyte Mac-1 and p150,95 adhesion proteins from an intracellular vesicular compartment to the cell surface.
Bainton, DF; Borregaard, N; Miller, LJ; Springer, TA, 1987
)
0.27
" Dose-response curves for chemiluminescence and beta-glucuronidase release are shifted to the left and maxima are increased."( Endotoxin pretreatment enhances neutrophil FMLP-receptor binding and activity in guinea pigs.
Bille-Hansen, V; Olsen, UB, 1987
)
0.27
" Millimolar Ca2+ alone was sufficient to stimulate [3H]InsP3 production; however, in the presence of guanosine 5'-[gamma-thio]triphosphate, the Ca2+ dose-response curve was shifted to submicromolar concentrations."( Guanine nucleotide regulation of phospholipase C activity in permeabilized rabbit neutrophils. Inhibition by pertussis toxin and sensitization to submicromolar calcium concentrations.
Bradford, PG; Rubin, RP, 1986
)
0.27
" No dose-response relationship was demonstrated."( In vitro locomotion of blood monocytes in millipore filters--evaluation of the leading front method.
Aasen, TB; Schreiner, A, 1986
)
0.27
" Monocyte adherence to microvascular endothelial cell monolayers was stimulated in a dose-response fashion in the presence of C5a des arg or FMLP to a maximum mean adherence of 47."( Human monocyte adherence: a primary effect of chemotactic factors on the monocyte to stimulate adherence to human endothelium.
Doherty, DE; Haslett, C; Henson, PM; Tonnesen, MG, 1987
)
0.27
" These results suggest that modulation of leukotaxis by NSAIDs may reflect a differential dose-response sensitivity of lipoxygenase and cycloxygenase pathways."( In vivo modulation of leukotaxis by non-steroidal anti-inflammatory drugs.
diZerega, GS; Nakamura, RM; Shimanuki, T, 1985
)
0.27
" Leukotrienes, the chemotactic fragment of the fifth component of complement (C5a des arg), N-formyl-L-methionylyl-L-leucyl-L-phenylalanine (FMLP), platelet-activating factor (PAF), and phorbol myristate acetate (PMA) increased the nonadherence of human leukocytes to glass with bell-shaped dose-response curves."( Various authentic chemoattractants mediating leukocyte adherence inhibition.
Thomson, DM, 1984
)
0.27
" The dose-response curve for the inhibition of binding was very similar to the dose-response curves for the inhibition of FMLP-induced neutrophil activation."( Sulfasalazine inhibition of binding of N-formyl-methionyl-leucyl-phenylalanine (FMLP) to its receptor on human neutrophils.
Mehta, J; Spilberg, I; Stenson, WF, 1984
)
0.27
" The relevance of this reaction to secretory phenomena is indicated by its requirement for Ca, its rapid onset, and dose-response curves that paralleled those of the secretory response."( Calcium-phospholipid interactions in secretory cells: a new perspective on stimulus-secretion coupling.
Rubin, RP, 1982
)
0.26
"The dose-response characteristics of the neutrophil 3-3'-dipentyloxacarbocyanine (di-O-C5(3)) fluorescence response to repetitive stimulation with the chemoattractant N-formylmethionylleucylphenylalanine (fMet-Leu-Phe) were studied."( Adaptation of human neutrophil responsiveness to the chemoattractant N-formylmethionylleucylphenylalanine. Heterogeneity and/or negative cooperative interaction of receptors.
Fletcher, MP; Gallin, JI; Seligmann, BE, 1982
)
0.26
" This secretory response was normal as judged by cell ultrastructure and FMLP dose-response relationships."( FMLP-induced enzyme release from neutrophils: a role for intracellular calcium.
Chandler, D; Meusel, G; Schumaker, E; Stapleton, C, 1983
)
0.27
" Dose-response curves were generated using such proinflammatory materials as formyl-methionyl-leucyl-phenylalanine, lipopolysaccharide, activated serum, trypsin, glycogen, and acetic acid."( Labeling of peripheral blood polymorphonuclear leukocytes with indium-111: a new method for the quantitation of in-vivo accumulation of PMNLs in rabbit skin.
Barnes, B; Lazarus, GS; Wahba, AV, 1984
)
0.27
" The signal for priming could be clearly distinguished from the signal causing oxidase activation by the dose-response curves for each, as well as by the use of several pharmacologic agents."( The NADPH oxidase of human polymorphonuclear leukocytes. Evidence for regulation by multiple signals.
Clayton, CC; McPhail, LC; Snyderman, R, 1984
)
0.27
" Neither the time course of the response nor the dose-response curve is affected by the removal of calcium from the suspending medium."( Stimulation by chemotactic factor of actin association with the cytoskeleton in rabbit neutrophils. Effects of calcium and cytochalasin B.
Naccache, PH; Sha'afi, RI; White, JR, 1983
)
0.27
" Dose-response experiments performed with 2 to 90 per cent (v/v) zymosan-activated plasma showed a direct correlation between the rate of neutrophil influx and the degree of vascular permeability in blood flow."( Vascular responses during acute neutrophilic inflammation. Their relationship to in vivo neutrophil emigration.
Issekutz, AC, 1981
)
0.26
" The cell dose-response was linear for both preparations over a wide range of cell concentrations in the cell input well of the chemotaxis chamber, suggesting that no monocyte-monocyte interaction was required."( Chemotaxis of purified human monocytes in vitro: lack of accessory cell requirement.
Falk, W; Leonard, EJ, 1982
)
0.26
" Dose-response curves to the synthetic chemotactic agent Formyl-Methionyl-Leucyl-Phenylalanine (FMLP) showed decreased response to submaximal chemokinetic stimuli in stored neutrophils."( Decreased affinity for a chemotactic factor in stored granulocyte concentrates.
Lane, TA; Windle, BE,
)
0.13
" Similar dose-response curves for esterase activation, chemotaxis, and chemotactic deactivation were obtained with the chemotactic factor FMLP, suggesting that in human neutrophils all three functions utilize some of the same early molecular events following chemotactic factor binding to th neutrophil surface."( Demonstration of calcium-dependent chemotactic factor activatable esterase activity in human neutrophils: relationship with chemotaxis and chemotactic deactivation.
Kleyman, T; Mandell, B; Mehta, J; Spilberg, I, 1981
)
0.26
" Dose-response studies under comparable conditions showed that aggregation is induced in similar dose ranges as chemotaxis."( Aggregation of leukocytes induced by the complement-derived peptides C3a and C5a and by three synthetic formyl-methionyl peptides.
Damerau, B; Grünefeld, E; Vogt, W, 1980
)
0.26
" Dose-response kinetics were similar to those of the chemotactic response."( Comparison of biological responses of human monocytes and THP-1 cells to chemokines of the intercrine-beta family.
Newton, RC; Vaddi, K, 1994
)
0.29
" Further studies indicated that monocyte binding to endothelial cells follows similar dose-response kinetics as the up-regulation of integrins and can be partially blocked by Abs to CD11b and CD11c."( Regulation of monocyte integrin expression by beta-family chemokines.
Newton, RC; Vaddi, K, 1994
)
0.29
" Dose-response analysis revealed that maximal reduction of IL-1 binding was reached at FMLP concentrations that were also optimal for chemotaxis (50% effective dose = 5 x 10(-9) M)."( Chemoattractants induce rapid release of the interleukin 1 type II decoy receptor in human polymorphonuclear cells.
Colotta, F; Fadlon, EJ; Mantovani, A; Matteucci, C; Orlando, S; Sozzani, S, 1995
)
0.29
" Biphasic dose-response curves of SW neutrophil adherence were observed using FMLP, but not using concanavalin A or phorbol myristate acetate as stimulatory agents."( Studies of skin-window exudate human neutrophils: complex patterns of adherence to serum-coated surfaces in dependence on FMLP doses.
Bambara, LM; Bellavite, P; Biasi, D; Caramaschi, P; Carletto, A; Poli, F; Suttora, F, 1994
)
0.29
" Dose-response curves were remarkably similar for all three compounds."( Methyl mercury, mercuric chloride, and silver lactate decrease superoxide anion formation and chemotaxis in human polymorphonuclear leucocytes.
Christensen, MM; Hansen, B; Nielsen, SL; Obel, N; Rungby, J, 1993
)
0.29
" By investigating the dose-response relationships of these phenomena, we have found that: (a) resting neutrophils do not produce a significant amount of superoxide (O2-) and show only minimal adhesion to serum-coated plastic surfaces; (b) fully activatory doses (> 5 x 10(-8) M) of fMLP induce the release of O2- and a significant increase of the cell adhesion; (c) pretreatment of the cells for 1 h with LPS augments cell adhesion to serum-coated culture wells in the absence of further stimulation and primes the neutrophils to enhanced fMLP-dependent O2- release; (d) addition of low, substimulatory doses of fMLP (from 10(-10) M to 5 x 10(-9) M) inhibits and reverses the adhesion of LPS-treated cells, (e) high fMLP doses ( > 10(-7) M) are additive to LPS in promoting adhesion."( Dual effects of formylpeptides on the adhesion of endotoxin-primed human neutrophils.
Andrioli, G; Bellavite, P; Bonazzi, L; Chirumbolo, S; Ferro, I; Lippi, G, 1993
)
0.29
"The dose-response relationship of commercially available preparations of methohexital, pentobarbital, phenobarbital, and thiopental and their respective drug-free solutions on granulocyte function was investigated to evaluate whether suppression of neutrophil chemiluminescence is mediated by the barbiturates themselves or by their drug-free solutions."( Do barbiturates impair zymosan-induced granulocyte function?
Birkhahn, A; Buhl, R; Mirow, N; Schneider, M; Weiss, M; Wernet, P, 1994
)
0.29
"The dose-response effects of the four barbiturates on granulocyte function were tested by zymosan-induced neutrophil chemiluminescence and, in addition, in a cell-free chemiluminescence system."( Do barbiturates impair zymosan-induced granulocyte function?
Birkhahn, A; Buhl, R; Mirow, N; Schneider, M; Weiss, M; Wernet, P, 1994
)
0.29
"The dose-response relationship of four commercially available barbiturates (methohexitone, pentobarbitone, phenobarbitone and thiopentone) and of their drug-free solutions on the production of oxygen radicals by neutrophils were tested by N-formylmethionyl-leucyl-phenylalanine (FMLP)-induced granulocyte chemiluminescence and in a cell-free chemiluminescence system."( Do barbiturates and their solutions suppress FMLP-induced neutrophil chemiluminescence?
Birkhahn, A; Buhl, R; Mirow, N; Schneider, M; Weiss, M; Wernet, P, 1994
)
0.29
" Terfenadine, at concentrations achievable at standard dosing regimens, has anti-inflammatory properties in vitro."( Effect of terfenadine on human eosinophil and neutrophil chemotactic response and generation of superoxide.
Eda, R; Hopp, RJ; Townley, RG, 1994
)
0.29
" The dose-response curves showed that tyrosine phosphorylation and O2- release were stimulated in parallel by PMA, whereas tyrosine phosphorylation and an increase in [Ca2+]i, but not O2- release, were stimulated in parallel by FMLP or ionomycin."( Activation of the respiratory burst and tyrosine phosphorylation of proteins in human neutrophils: no direct relationship and involvement of protein kinase C-dependent and -independent signaling pathways.
Azuma, EK; Kitagawa, S; Mizoguchi, H; Saito, M; Takaku, F; Umezawa, K; Yuo, A, 1993
)
0.29
" Dose-response curves of the calcium response were determined by measuring the fluorescence of neutrophils loaded with fura-2 and stimulated with various concentrations of the chemotactic tripeptide formylmethionylleucylphenylalanine."( Increased sensitivity to agonist stimulation of the Ca2+ response in neutrophils of manic-depressive patients: effect of lithium therapy.
Berger, M; Bohus, M; Förstner, U; Gebicke-Härter, P; Hecht, H; van Calker, D; Wark, HJ, 1993
)
0.29
" Pharmacokinetic studies indicate that after oral dosing L-680,833 is bioavailable in rats and rhesus monkeys."( Chemical, biochemical, pharmacokinetic, and biological properties of L-680,833: a potent, orally active monocyclic beta-lactam inhibitor of human polymorphonuclear leukocyte elastase.
Brause, K; Chandler, GO; Doherty, JB; Dorn, CP; Finke, PE; Hagmann, WK; Hale, JJ; Kissinger, AL; Shah, SK; Thompson, KR, 1993
)
0.29
" The effects of PDE were dose dependent over the range of 10-70% (v/v) and simply augmented and reduced the dose-response curve to fMLP and PMA, respectively."( Effect of peritoneal dialysis effluent on superoxide anion production by polymorphonuclear neutrophils.
Daniels, I; Fletcher, J; Haynes, AP; Lindsay, M; Morgan, AG; Porter, C, 1993
)
0.29
" LC1 was approximately 200 times more potent than Ac2-26 on a molar basis although both gave maximal inhibitions, in contrast fragment 1-188 only produced a partial dose-response curve."( Lipocortin-1 fragments inhibit neutrophil accumulation and neutrophil-dependent edema in the mouse. A qualitative comparison with an anti-CD11b monoclonal antibody.
Ahluwalia, A; Flower, RJ; Goulding, NJ; Harris, JG; Perretti, M, 1993
)
0.29
" FMLP-stimulated CD11b upregulation as well as homotypic aggregation of PMN was inhibited by LXA4 (which at 10(-9) M gave approximately 1 log unit shift to the right in the FMLP dose-response curve)."( 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.
Fiore, S; Serhan, CN, 1995
)
0.29
" The dose-response curves of histamine release induced by the above stimuli were similar in SSc patients (n=15) and in normal subjects (n=39)."( Impairment of the inhibitory effect of sodium on basophil histamine release in patients with systemic sclerosis.
Mascagni, B; Miadonna, A; Milazzo, N; Palella, M; Tedeschi, A, 1996
)
0.29
" The priming effect of MCAF was maximal within 5 minutes of preincubation, and the dose-response curves for priming were identical to those for triggering of an increase in [Ca2+]i."( Activation and priming of human monocytes by monocyte chemotactic activating factor: cooperation with other inflammatory cytokines and close association between an increase in cytoplasmic free Ca2+ and intracellular acidification.
Azuma, EK; Kasahara, T; Kitagawa, S; Matsushima, T; Mizoguchi, H; Saito, M; Takaku, F; Yuo, A, 1996
)
0.29
" While fMLP exerted similar effects in both populations, dose-response curves for SP1 NKA and the NK2 receptor agonist were shifted leftwards (1, 4 and 3 orders of magnitude, respectively) in sensitized AMs."( Modulation by protein kinase C of the enhanced responsiveness to tachykinins in ovalbumin-sensitized guinea pig alveolar macrophages.
Brunelleschi, S; Fantozzi, R; Guidotto, S; Tonso, E; Viano, I, 1996
)
0.29
" There was a bell-shaped dose-response curve to the enhancing effects of HNE, depending on the incubation time being recorded after only short periods (< or = 5 min) of the exposure of the cells to HNE; this was not shown by structurally-related aldehydes, such as 2-nonenal and nonanal."( Effect of 4-hydroxynonenal on superoxide anion production from primed human neutrophils.
Dianzani, C; Fantozzi, R; Ferrara, C; Parrini, M, 1996
)
0.29
" However, since the optimal dose, the dosing interval, and the mechanisms of action are not well-defined, we studied the effects on CGD neutrophil (PMN) functions ex vivo of interferon-gamma (IFN-gamma)."( Dose-dependent enhancements by interferon-gamma on functional responses of neutrophils from chronic granulomatous disease patients.
Ahlin, A; Elinder, G; Palmblad, J, 1997
)
0.3
" However, a rightward shift was observed in the dose-response curve of N-formyl-methionyl-leucyl-phenylalanine-stimulated BDR neutrophil O2- production."( Impaired neutrophil microbicidal activity in rat cholestasis.
Swain, MG; Tjandra, K; Woodman, RC, 1997
)
0.3
" For these patients orally administered pentoxifylline failed to decrease reactive oxygen species generation by spermatozoa, and had no effect on sperm motility, sperm motion parameters and sperm fertilizing ability at low dosage (300 mg."( Formation of reactive oxygen species by spermatozoa from asthenospermic patients: response to treatment with pentoxifylline.
Arakawa, S; Fujisawa, M; Kamidono, S; Kanzaki, M; Okada, H; Tatsumi, N, 1997
)
0.3
" Orally administered pentoxifylline had no effect at low dosage but it increased sperm motility and some sperm motion parameters without altering sperm fertilizing ability at high dosage."( Formation of reactive oxygen species by spermatozoa from asthenospermic patients: response to treatment with pentoxifylline.
Arakawa, S; Fujisawa, M; Kamidono, S; Kanzaki, M; Okada, H; Tatsumi, N, 1997
)
0.3
" In transfected cells, dissociation of ligand is sensitive to guanine nucleotide, the G protein is pertussis toxin-sensitive, FPR and G protein appear to be precoupled, the F-actin response is stimulated with the same dose-response profile as in neutrophils, and the F-actin accumulation response is directly regulated by the FPR, even long after initial stimulation."( Relationship of ligand-receptor dynamics to actin polymerization in RBL-2H3 cells transfected with the human formyl peptide receptor.
Hall, AL; Oliver, JM; Pfeiffer, JR; Sklar, LA; Wilson, BS, 1997
)
0.3
" The growth factor was administered subcutaneously for five days in a dosage of 5 microg/Kg/day."( fMLP-induced CD11b/CD18 upregulation on neutrophils from patients with non-Hodgkin's lymphomas treated with recombinant human granulocyte colony-stimulating factor.
Ambrogi, F; Angiolini, C; Azzarà, A; Carulli, G; Minnucci, S; Sbrana, S, 1997
)
0.3
" The slope and the shape of the dose-response curve of DEX were similar irrespective of either the input stimuli or the output cytokines; half-maximal inhibition was observed at 10(-8) mol/L, and nearly complete abolishment was observed at 10(-7) mol/L."( Glucocorticoids inhibit chemokine generation by human eosinophils.
Hirai, K; Izumi, S; Kasahara, T; Matsushima, K; Misaki, Y; Miyamasu, M; Morita, Y; Nakamura, H; Takaishi, T, 1998
)
0.3
" A dose-response test was also conducted for extracellular calcium."( Chemoattractant- and mitogen-induced generation of reactive oxygen species in human lymphocytes: the role of calcium.
Orie, NN; Tepel, M; Zidek, W, 1999
)
0.3
" MT, like PMA, evoked a leftward shift of the dose-response curve for the STZ-induced [Ca(2)+](i) rise, indicating PKC-dependent sensitization of neutrophils for stimulation by STZ."( Nutritional lipid emulsions modulate cellular signaling and activation of human neutrophils.
Naber, T; van Emst-De Vries, S; Wanten, G; Willems, P, 2001
)
0.31
" The competitive antagonistic action was further confirmed by the finding that rebamipide caused a parallel shift to the right in the dose-response curve of O2 production induced by fMLP."( Rebamipide suppresses formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide production by inhibiting fMLP-receptor binding in human neutrophils.
Azuma, A; Imagawa, K; Ishiyama, H; Kikuchi, M; Nagano, C; Sekiguchi, K, 2001
)
0.31
" GCSF at a dosage of 30 to 100 ng/mL, a concentration range that primes superoxide release, stimulated a 60% to 100% increase in gelatinase release from tertiary granules but did not stimulate lactoferrin release from secondary granules."( Granulocyte colony-stimulating factor primes NADPH oxidase in neutrophils through translocation of cytochrome b(558) by gelatinase-granule release.
Boxer, LA; Hinkovska-Galcheva, V; Mansfield, PJ; Shayman, JA, 2002
)
0.31
" The fMLP-stimulated production of superoxide anion (O(2)(-)) showed a sigmoidal-shaped fMLP dose-response curve, and constant O(2)(-) production rates (nmol."( Cryopreservation of reduced cytochrome C for determination of N-formyl-methionyl-leucyl-phenylalanine-stimulated superoxide anion production in human whole blood.
Choukèr, A; Christ, F; DaSilva, L; Diem, H; Martignoni, A; Peter, K; Thiel, M, 2002
)
0.31
"A biphasic dose-response curve emerged for both the neutrophil spontaneous random migration and the fMLP-induced chemotaxis."( Hemin, a heme oxygenase substrate analog, both inhibits and enhances neutrophil random migration and chemotaxis.
Andersson, JA; Cardell, LO; Uddman, R, 2002
)
0.31
" The 1,3,5-triazines tested inhibited the adhesion evoked by pro-inflammatory stimuli, such as platelet activating factor (PAF), FMLP, phorbol myristate acetate (PMA), tumour necrosis factor-alpha (TNF-alpha) and interleukin-1beta(IL-1beta) in a dose-response manner over the concentration range 10(-9) to 10(-4)M, compounds 5 and 6 being the most active."( Evaluation of in-vitro anti-inflammatory activity of some 2-alkyl-4,6-dimethoxy-1,3,5-triazines.
Collino, M; Dianzani, C; Fantozzi, R; Gallicchio, M; Menicagli, R; Samaritani, S; Signore, G, 2006
)
0.33
" This is the first systematic dose-response evaluation of soluble stimulants of neutrophil respiratory burst in rats."( Flow-cytometric measurement of respiratory burst in rat polymorphonuclear granulocytes: Comparison of four cell preparation procedures, and concentration-response evaluation of soluble stimulants.
Bitzinger, DI; Dittmar, MS; Lindner, R; Schlachetzki, F; Trabold, B, 2008
)
0.35
" For OB assays, dose-response curves were performed for each activator."( Oxidative burst assessment and neutrophil-platelet complexes in unlysed whole blood.
Avendaño, A; Marin, L; Marin, P; Petriz, J; Sales-Pardo, I, 2008
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
tripeptideAny oligopeptide that consists of three amino-acid residues connected by peptide linkages.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (9)

PathwayProteinsCompounds
Signaling Pathways1269117
Signaling by GPCR24955
GPCR ligand binding19339
Class A/1 (Rhodopsin-like receptors)16136
Peptide ligand-binding receptors973
Formyl peptide receptors bind formyl peptides and many other ligands31
GPCR downstream signalling17252
G alpha (i) signalling events8741
Complement system02

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency79.43280.044717.8581100.0000AID485294
thioredoxin reductaseRattus norvegicus (Norway rat)Potency89.12510.100020.879379.4328AID588453
thioredoxin glutathione reductaseSchistosoma mansoniPotency50.11870.100022.9075100.0000AID485364
chromobox protein homolog 1Homo sapiens (human)Potency79.43280.006026.168889.1251AID540317
gemininHomo sapiens (human)Potency31.62280.004611.374133.4983AID624297
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
fMet-Leu-Phe receptorHomo sapiens (human)IC50 (µMol)0.02000.02004.006710.0000AID219067
fMet-Leu-Phe receptorHomo sapiens (human)Ki0.04200.04200.07100.1000AID290716
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
fMet-Leu-Phe receptorHomo sapiens (human)EC50 (µMol)0.01500.00250.01210.0200AID428657; AID91146
fMet-Leu-Phe receptorHomo sapiens (human)Kd0.00300.00300.11650.2300AID1196961
N-formyl peptide receptor 2Homo sapiens (human)EC50 (µMol)20.40000.00250.01250.0190AID428658
FML2_HUMAN Homo sapiens (human)EC50 (µMol)1.90001.90001.90001.9000AID428659
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (23)

Processvia Protein(s)Taxonomy
phospholipase C-activating G protein-coupled receptor signaling pathwayfMet-Leu-Phe receptorHomo sapiens (human)
chemotaxisfMet-Leu-Phe receptorHomo sapiens (human)
signal transductionfMet-Leu-Phe receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayfMet-Leu-Phe receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayfMet-Leu-Phe receptorHomo sapiens (human)
nitric oxide mediated signal transductionfMet-Leu-Phe receptorHomo sapiens (human)
complement receptor mediated signaling pathwayfMet-Leu-Phe receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationfMet-Leu-Phe receptorHomo sapiens (human)
inflammatory responsefMet-Leu-Phe receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayfMet-Leu-Phe receptorHomo sapiens (human)
immune response-regulating cell surface receptor signaling pathwayN-formyl peptide receptor 2Homo sapiens (human)
chemotaxisN-formyl peptide receptor 2Homo sapiens (human)
cell adhesionN-formyl peptide receptor 2Homo sapiens (human)
cell surface receptor signaling pathwayN-formyl peptide receptor 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayN-formyl peptide receptor 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayN-formyl peptide receptor 2Homo sapiens (human)
calcium-mediated signalingN-formyl peptide receptor 2Homo sapiens (human)
positive regulation of superoxide anion generationN-formyl peptide receptor 2Homo sapiens (human)
defense response to bacteriumN-formyl peptide receptor 2Homo sapiens (human)
positive regulation of innate immune responseN-formyl peptide receptor 2Homo sapiens (human)
negative regulation of inflammatory responseN-formyl peptide receptor 2Homo sapiens (human)
positive regulation of phagocytosisN-formyl peptide receptor 2Homo sapiens (human)
positive chemotaxisN-formyl peptide receptor 2Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeN-formyl peptide receptor 2Homo sapiens (human)
positive regulation of monocyte chemotaxisN-formyl peptide receptor 2Homo sapiens (human)
cellular response to amyloid-betaN-formyl peptide receptor 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayN-formyl peptide receptor 2Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationN-formyl peptide receptor 2Homo sapiens (human)
inflammatory responseN-formyl peptide receptor 2Homo sapiens (human)
complement receptor mediated signaling pathwayN-formyl peptide receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
G protein-coupled receptor bindingfMet-Leu-Phe receptorHomo sapiens (human)
G protein-coupled receptor activityfMet-Leu-Phe receptorHomo sapiens (human)
N-formyl peptide receptor activityfMet-Leu-Phe receptorHomo sapiens (human)
scavenger receptor bindingfMet-Leu-Phe receptorHomo sapiens (human)
protein bindingfMet-Leu-Phe receptorHomo sapiens (human)
RAGE receptor bindingfMet-Leu-Phe receptorHomo sapiens (human)
complement receptor activityfMet-Leu-Phe receptorHomo sapiens (human)
amyloid-beta bindingN-formyl peptide receptor 2Homo sapiens (human)
G protein-coupled receptor activityN-formyl peptide receptor 2Homo sapiens (human)
scavenger receptor bindingN-formyl peptide receptor 2Homo sapiens (human)
protein bindingN-formyl peptide receptor 2Homo sapiens (human)
signaling receptor activityN-formyl peptide receptor 2Homo sapiens (human)
complement receptor activityN-formyl peptide receptor 2Homo sapiens (human)
N-formyl peptide receptor activityN-formyl peptide receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
cytoplasmfMet-Leu-Phe receptorHomo sapiens (human)
plasma membranefMet-Leu-Phe receptorHomo sapiens (human)
membranefMet-Leu-Phe receptorHomo sapiens (human)
secretory granule membranefMet-Leu-Phe receptorHomo sapiens (human)
azurophil granule membranefMet-Leu-Phe receptorHomo sapiens (human)
ficolin-1-rich granule membranefMet-Leu-Phe receptorHomo sapiens (human)
plasma membranefMet-Leu-Phe receptorHomo sapiens (human)
cytoplasmN-formyl peptide receptor 2Homo sapiens (human)
plasma membraneN-formyl peptide receptor 2Homo sapiens (human)
membraneN-formyl peptide receptor 2Homo sapiens (human)
specific granule membraneN-formyl peptide receptor 2Homo sapiens (human)
tertiary granule membraneN-formyl peptide receptor 2Homo sapiens (human)
ficolin-1-rich granule membraneN-formyl peptide receptor 2Homo sapiens (human)
plasma membraneN-formyl peptide receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (37)

Assay IDTitleYearJournalArticle
AID1196962Binding affinity to human FPR2 receptor2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Pachymodulin, a new functional formyl peptide receptor 2 peptidic ligand isolated from frog skin has Janus-like immunomodulatory capacities.
AID1196961Binding affinity to human FPR1 receptor2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Pachymodulin, a new functional formyl peptide receptor 2 peptidic ligand isolated from frog skin has Janus-like immunomodulatory capacities.
AID1196968Induction of fLMP-induced migration in human neutrophils preincubated at 10 uM after 45 mins by chemotaxis assay2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Pachymodulin, a new functional formyl peptide receptor 2 peptidic ligand isolated from frog skin has Janus-like immunomodulatory capacities.
AID1348474Induction of cell migration in rat RBL2H3/ETFR cells stably expressing FPR1 at 10 nM after 6 hrs by RTCA2018European journal of medicinal chemistry, Jan-01, Volume: 143Urokinase receptor derived peptides as potent inhibitors of the formyl peptide receptor type 1-triggered cell migration.
AID428657Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
6-methyl-2,4-disubstituted pyridazin-3(2H)-ones: a novel class of small-molecule agonists for formyl peptide receptors.
AID1348476Inhibition of FITC-fMLF induced FPR1 internalization in rat RBL-2H3/ETFR cells at 10 uM preincubated for 30 mins followed by agonist addition measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Urokinase receptor derived peptides as potent inhibitors of the formyl peptide receptor type 1-triggered cell migration.
AID1348478Inhibition of FITC-fMLF induced FPR1 internalization in rat RBL-2H3/ETFR cells at 10 uM preincubated for 30 mins followed by agonist addition measured after 30 mins by confocal fluorescent microscopy2018European journal of medicinal chemistry, Jan-01, Volume: 143Urokinase receptor derived peptides as potent inhibitors of the formyl peptide receptor type 1-triggered cell migration.
AID290716Displacement of [3H]-fMLP from FPR in human neutrophils2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
2-Phenyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives: new potent inhibitors of fMLP-induced neutrophil chemotaxis.
AID1196976Induction of calcium release in human FPR2 receptor-expressed HEK cell at 10 uM measured after second challenge by cytosolic-free calcium assay2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Pachymodulin, a new functional formyl peptide receptor 2 peptidic ligand isolated from frog skin has Janus-like immunomodulatory capacities.
AID680861TP_TRANSPORTER: inhibition of Gly-Sar uptake (Gly-Sar: 100 uM, fMLP: 1000 uM) in Xenopus laevis oocytes1998The Journal of clinical investigation, Dec-01, Volume: 102, Issue:11
hPepT1-mediated epithelial transport of bacteria-derived chemotactic peptides enhances neutrophil-epithelial interactions.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1196977Induction of calcium release in human FPR2 receptor-expressed HEK cell assessed as calcium release through Cav1.2 channel at 10 uM by cytosolic-free calcium assay in presence of 30 uM ATP2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Pachymodulin, a new functional formyl peptide receptor 2 peptidic ligand isolated from frog skin has Janus-like immunomodulatory capacities.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID91146Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils1996Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
N-terminus urea-substituted chemotactic peptides: new potent agonists and antagonists toward the neutrophil fMLF receptor.
AID680652TP_TRANSPORTER: uptake in Xenopus laevis oocytes1998The Journal of clinical investigation, Dec-01, Volume: 102, Issue:11
hPepT1-mediated epithelial transport of bacteria-derived chemotactic peptides enhances neutrophil-epithelial interactions.
AID1196963Binding affinity to mouse FPR2 receptor2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Pachymodulin, a new functional formyl peptide receptor 2 peptidic ligand isolated from frog skin has Janus-like immunomodulatory capacities.
AID428659Agonist activity at FPRL2 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
6-methyl-2,4-disubstituted pyridazin-3(2H)-ones: a novel class of small-molecule agonists for formyl peptide receptors.
AID219067Binding affinity towards fMLF receptor using human neutrophils1996Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
N-terminus urea-substituted chemotactic peptides: new potent agonists and antagonists toward the neutrophil fMLF receptor.
AID428658Agonist activity at FPRL1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
6-methyl-2,4-disubstituted pyridazin-3(2H)-ones: a novel class of small-molecule agonists for formyl peptide receptors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1345847Mouse FPR1 (Formylpeptide receptors)2008Journal of immunology (Baltimore, Md. : 1950), Jul-15, Volume: 181, Issue:2
Identification of formyl peptides from Listeria monocytogenes and Staphylococcus aureus as potent chemoattractants for mouse neutrophils.
AID1345827Human FPR1 (Formylpeptide receptors)1976The Journal of experimental medicine, May-01, Volume: 143, Issue:5
The structure-activity relations of synthetic peptides as chemotactic factors and inducers of lysosomal secretion for neutrophils.
AID1345806Human FPR2/ALX (Leukotriene receptors)1993The Journal of biological chemistry, Aug-25, Volume: 268, Issue:24
Multiple domains of the N-formyl peptide receptor are required for high-affinity ligand binding. Construction and analysis of chimeric N-formyl peptide receptors.
AID1345827Human FPR1 (Formylpeptide receptors)1980Biochemistry, May-27, Volume: 19, Issue:11
Further studies on the structural requirements for synthetic peptide chemoattractants.
AID1345847Mouse FPR1 (Formylpeptide receptors)1999The Journal of experimental medicine, Sep-06, Volume: 190, Issue:5
N-formylpeptides induce two distinct concentration optima for mouse neutrophil chemotaxis by differential interaction with two N-formylpeptide receptor (FPR) subtypes. Molecular characterization of FPR2, a second mouse neutrophil FPR.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6,511)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901808 (27.77)18.7374
1990's3055 (46.92)18.2507
2000's1219 (18.72)29.6817
2010's395 (6.07)24.3611
2020's34 (0.52)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials53 (0.79%)5.53%
Reviews99 (1.47%)6.00%
Case Studies41 (0.61%)4.05%
Observational0 (0.00%)0.25%
Other6,523 (97.13%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]