A truncated form of CKbeta8-1 is a potent agonist for human formyl peptide-receptor-like 1 receptor.

Abstract:

:1. Human formyl peptide-receptor-like-1 (FPRL-1) is a promiscuous G protein-coupled receptor (GPCR), and belongs to a chemoattractant receptor family protein. This receptor has been reported to interact with various host-derived peptides and lipids involved in inflammatory responses. We described here, a novel role for FPRL-1 as a high-affinity beta-chemokine receptor for an N-terminally truncated form of the CKbeta8 (CCL23/MPIF-1) splice variant CKbeta8-1 (22-137 aa). 2. RT-PCR analysis of mRNA derived from human tissues and cells revealed a predominant expression of FPRL-1 in inflammatory cells, particularly in neutrophils. 3. Intracellular calcium mobilisation assay, used as screening tool, in recombinant Chinese hamster ovary (CHO-K1) and human embryonic kidney (HEK293s) cells coexpressing FPRL-1 and Galpha(16), demonstrated FPRL-1 is a functional high-affinity receptor for CKbeta8-1 (46-137 aa, sCKbeta8-1), with pEC(50) values of 9.13 and 8.85, respectively. 4. The FPRL-1 activation in CHO-K1 cells is mediated by Galpha(i)/Galpha(o) proteins, as assessed by pertussis toxin sensitivity and inhibition of forskolin-induced cyclic AMP accumulation. 5. Binding experiments were performed with a radio-iodinated synthetic peptide, [(125-)I]-WKYMVm, a known potent FPRL-1 agonist. CHO-K1 cell membranes expressing FPRL-1 bound [(125-)I]-WKYMVm with a K(d) value of 9.34. Many known FPRL-1 agonists were tested and sCKbeta8-1 was the most effective nonsynthetic ligand in displacing the radiolabelled agonist, with a pIC(50) of 7.97. 6. The functional significance of sCKbeta8-1 interaction with FPRL-1 was further demonstrated by the activation of polymorphonuclear leukocytes (PMNs) calcium mobilisation and chemotaxis. These interactions were shown to be via FPRL-1 by specific blockade of PMNs activation in the presence of an FPRL-1 antibody.

journal_name

Br J Pharmacol

authors

Elagoz A,Henderson D,Babu PS,Salter S,Grahames C,Bowers L,Roy MO,Laplante P,Grazzini E,Ahmad S,Lembo PM

doi

10.1038/sj.bjp.0705592

subject

Has Abstract

pub_date

2004-01-01 00:00:00

pages

37-46

issue

1

eissn

0007-1188

issn

1476-5381

pii

sj.bjp.0705592

journal_volume

141

pub_type

杂志文章
  • Investigation of the maternal to foetal serum concentration gradient of dexamethasone in the rat.

    abstract::The basis of the maternal to foetal serum concentration gradient of dexamethasone was investigated in the rat on day 20 of gestation. The pregnant rat was assumed to behave as a two-compartment open model with one maternal and one foetal pool exchanging with each other and each to outside. Bolus injections of unlabell...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1986.tb16254.x

    authors: Varma DR

    更新日期:1986-08-01 00:00:00

  • Stimulation of rat erythrocyte P2X7 receptor induces the release of epoxyeicosatrienoic acids.

    abstract:BACKGROUND AND PURPOSE:Red blood cells (RBCs) are reservoirs of vasodilatory, antiaggregatory, and antiinflammatory lipid mediators-epoxyeicosatrienoic acids (EETs). This study addresses the formation and release of erythrocyte-derived EETs in response to ATP receptor stimulation that may represent an important mechani...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0707311

    authors: Jiang H,Zhu AG,Mamczur M,Falck JR,Lerea KM,McGiff JC

    更新日期:2007-08-01 00:00:00

  • Comparison of effect of morphine-like analgesics on transmurally stimulated guinea-pig ileum.

    abstract::1. Morphine-like analgesic drugs caused depression of twitches of the isolated guinea-pig ileum in response to transmural electrical stimulation. The drugs tested were the narcotic analgesics codeine, diamorphine, fentanyl, morphine, morphine-N-oxide, normorphine, oxymorphone, pethidine, phenazocine and phenoperidine ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1969.tb10580.x

    authors: Fennessy MR,Heimans RL,Rand MJ

    更新日期:1969-10-01 00:00:00

  • Shadows across mu-Star? Constitutively active mu-opioid receptors revisited.

    abstract::Constitutively active mu-opioid receptors (mu* receptors) are reported to be formed following prolonged agonist treatment of cells or whole animals. mu* receptors signal in the absence of activating ligand and a blockade of mu* activation of G-proteins by naloxone and naltrexone has been suggested to underlie the prof...

    journal_title:British journal of pharmacology

    pub_type: 评论,杂志文章

    doi:10.1111/j.1476-5381.2009.00067.x

    authors: Connor M

    更新日期:2009-04-01 00:00:00

  • Discovery, characterization and clinical utility of prostaglandin agonists for the treatment of glaucoma.

    abstract::Topical ophthalmic formulations of analogues of the endogenous arachidonic acid cyclooxygenase metabolite, PGF2α , are the standard of care treatment for the blinding disease glaucoma. These are the most potent and efficacious medical therapies for lowering intraocular pressure (IOP), the most important risk factor id...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.14327

    authors: Klimko PG,Sharif NA

    更新日期:2019-04-01 00:00:00

  • Inhibition of carrageenin-induced rat paw oedema by crotapotin, a polypeptide complexed with phospholipase A2.

    abstract::1. The effect of purified crotapotin, a non-toxic non-enzymatic chaperon protein normally complexed to a phospholipase A2 (PLA2) in South America rattlesnake venom, was studied in the acute inflammatory response induced by carrageenin (1 mg/paw), compound 48/80 (3 micrograms/paw) and 5-hydroxytryptamine (5-HT) (3 micr...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb17178.x

    authors: Landucci EC,Antunes E,Donato JL,Faro R,Hyslop S,Marangoni S,Oliveira B,Cirino G,de Nucci G

    更新日期:1995-02-01 00:00:00

  • Inhibition of rat platelet aggregation by the diazeniumdiolate nitric oxide donor MAHMA NONOate.

    abstract::1. Inhibition of rat platelet aggregation by the nitric oxide (NO) donor MAHMA NONOate (Z-1-N-methyl-N-[6-(N-methylammoniohexyl)amino]diazen-1-ium-1,2-diolate) was investigated. The aims were to compare its anti-aggregatory effect with vasorelaxation, to determine the effects of the soluble guanylate cyclase inhibitor...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0704971

    authors: Homer KL,Wanstall JC

    更新日期:2002-12-01 00:00:00

  • Differential classification of vascular smooth muscle and endothelial cell 5-HT receptors by use of tryptamine analogues.

    abstract::In ring preparations of the rabbit external jugular vein contracted with the thromboxane-mimetic U-46619, submicromolar concentrations of 5-hydroxytryptamine (5-HT) and chemically related analogues produced relaxations that were dependent on the integrity of the vascular endothelium. The receptor mediating endothelium...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1987.tb10287.x

    authors: Leff P,Martin GR,Morse JM

    更新日期:1987-06-01 00:00:00

  • CL/RAMP2 and CL/RAMP3 produce pharmacologically distinct adrenomedullin receptors: a comparison of effects of adrenomedullin22-52, CGRP8-37 and BIBN4096BS.

    abstract::Adrenomedullin (AM) has two known receptors formed by the calcitonin receptor-like receptor (CL) and receptor activity-modifying protein (RAMP) 2 or 3: we report the effects of the antagonist fragments of human AM and CGRP (AM22-52 and CGRP8-37) in inhibiting AM at human (h), rat (r) and mixed species CL/RAMP2 and CL/...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705472

    authors: Hay DL,Howitt SG,Conner AC,Schindler M,Smith DM,Poyner DR

    更新日期:2003-10-01 00:00:00

  • Relief learning is dependent on NMDA receptor activation in the nucleus accumbens.

    abstract:BACKGROUND AND PURPOSE:Recently, we demonstrated that the nucleus accumbens (NAC) is required for the acquisition and expression of relief memory. The purpose of this study was to investigate the role of NMDA receptors within the NAC in relief learning. EXPERIMENTAL APPROACH:The NMDA receptor antagonist 2-amino-5-phos...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13070

    authors: Mohammadi M,Fendt M

    更新日期:2015-05-01 00:00:00

  • A microdialysis study of the novel antiepileptic drug levetiracetam: extracellular pharmacokinetics and effect on taurine in rat brain.

    abstract::Using a rat model which allows serial blood sampling and concurrent brain microdialysis sampling, we have investigated the temporal kinetic inter-relationship of levetiracetam in serum and brain extracellular fluid (frontal cortex and hippocampus) following systemic administration of levetiracetam, a new antiepileptic...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0704141

    authors: Tong X,Patsalos PN

    更新日期:2001-07-01 00:00:00

  • Naloxone prevents cell-mediated immune alterations in adult mice following repeated mild stress in the neonatal period.

    abstract::1. Mild stress plus mild pain (solvent injection) applied daily to neonatal mice induces hormonal, behavioural and metabolic changes perduring in the adult life. 2. We investigated whether daily mild stress to neonatal mice induces also long-term defined changes of immune response, and whether immune changes are preve...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0704577

    authors: Loizzo A,Loizzo S,Lopez L,d'Amore A,Renzi P,Spampinato S,Di Carlo S,Bacosi A,Zuccaro P,Pacifici R

    更新日期:2002-03-01 00:00:00

  • Some observations on the estimation of 3-methoxytyramine in brain tissue.

    abstract::1. A new method for the estimation of 4-hydroxy-3-methoxyphenylethylamine (3-methoxytyramine) in brain tissue is described. This is based on the formation of a fluorescent derivative by oxidation with potassium ferricyanide in ammonium hydroxide solution.2. The effects of some drugs on the concentration of 3-methoxyty...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1971.tb07136.x

    authors: Guldberg HC,Sharman DF,Tegerdine PR

    更新日期:1971-08-01 00:00:00

  • Effects of hydrogen sulphide on motility patterns in the rat colon.

    abstract:BACKGROUND AND PURPOSE:Hydrogen sulphide (H2 S) is an endogenous gaseous signalling molecule with putative functions in gastrointestinal motility regulation. Characterization of H2 S effects on colonic motility is crucial to establish its potential use as therapeutic agent in the treatment of colonic disorders. EXPERI...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12100

    authors: Gil V,Parsons S,Gallego D,Huizinga J,Jimenez M

    更新日期:2013-05-01 00:00:00

  • Andrographolide protects against cigarette smoke-induced oxidative lung injury via augmentation of Nrf2 activity.

    abstract:BACKGROUND AND PURPOSE:Cigarette smoke is a major cause for chronic obstructive pulmonary disease (COPD). Andrographolide is an active biomolecule isolated from the plant Andrographis paniculata. Andrographolide has been shown to activate nuclear factor erythroid-2-related factor 2 (Nrf2), a redox-sensitive antioxidant...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12054

    authors: Guan SP,Tee W,Ng DS,Chan TK,Peh HY,Ho WE,Cheng C,Mak JC,Wong WS

    更新日期:2013-04-01 00:00:00

  • Potent vasoconstrictor actions of cyclopiazonic acid and thapsigargin on femoral arteries from spontaneously hypertensive rats.

    abstract::1. Ca2+ buffering function of sarcoplasmic reticulum (SR) in the resting state of arteries from spontaneously hypertensive rats (SHR) was examined. Differences in the effects of cyclopiazonic acid (CPA) and thapsigargin, agents which inhibit the Ca(2+)-ATPase of SR, on tension and cellular Ca2+ level were assessed in ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0700857

    authors: Nomura Y,Asano M,Ito K,Uyama Y,Imaizumi Y,Watanabe M

    更新日期:1997-01-01 00:00:00

  • The electro-mechanical window in anaesthetized guinea pigs: a new marker in screening for Torsade de Pointes risk.

    abstract:BACKGROUND AND PURPOSE:QT prolongation is commonly used as a surrogate marker for Torsade de Pointes (TdP) risk of non-cardiovascular drugs. However, use of this indirect marker often leads to misinterpretation of the realistic TdP risk, as tested compounds may cause QT prolongation without evoking TdP in humans. A neg...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2011.01795.x

    authors: Guns PJ,Johnson DM,Van Op den Bosch J,Weltens E,Lissens J

    更新日期:2012-05-01 00:00:00

  • The role of the PDE4D cAMP phosphodiesterase in the regulation of glucagon-like peptide-1 release.

    abstract:BACKGROUND AND PURPOSE:Increases in intracellular cyclic AMP (cAMP) augment the release/secretion of glucagon-like peptide-1 (GLP-1). As cAMP is hydrolysed by cAMP phosphodiesterases (PDEs), we determined the role of PDEs and particularly PDE4 in regulating GLP-1 release. EXPERIMENTAL APPROACH:GLP-1 release, PDE expre...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2009.00194.x

    authors: Ong WK,Gribble FM,Reimann F,Lynch MJ,Houslay MD,Baillie GS,Furman BL,Pyne NJ

    更新日期:2009-06-01 00:00:00

  • Extracellular ATP and UTP activate the protein kinase B/Akt cascade via the P2Y(2) purinoceptor in renal mesangial cells.

    abstract::Extracellular nucleotides can activate a common purinoceptor mediating various cell responses. In this study we report that stimulation of rat mesangial cells with ATP and UTP leads to a rapid activation of the protein kinase B/Akt (PKB) pathway. Time-course studies reveal a rapid and transient phosphorylation of both...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0704748

    authors: Huwiler A,Rölz W,Dorsch S,Ren S,Pfeilschifter J

    更新日期:2002-06-01 00:00:00

  • Regulation of Wnt/β-catenin signalling by tankyrase-dependent poly(ADP-ribosyl)ation and scaffolding.

    abstract::The Wnt/β-catenin signalling pathway is pivotal for stem cell function and the control of cellular differentiation, both during embryonic development and tissue homeostasis in adults. Its activity is carefully controlled through the concerted interactions of concentration-limited pathway components and a wide range of...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.14038

    authors: Mariotti L,Pollock K,Guettler S

    更新日期:2017-12-01 00:00:00

  • Pharmacological prevention of cardiovascular aging--targeting the Maillard reaction.

    abstract::The development of myocardial and large vessel stiffness with aging underlies the development of diastolic heart failure and isolated systolic hypertension. Nonenzymatic reaction between glucose and proteins (Maillard reaction) leading to collagen crosslinking in the myocardium and arterial wall has been implicated in...

    journal_title:British journal of pharmacology

    pub_type: 评论,杂志文章

    doi:10.1038/sj.bjp.0705832

    authors: Aronson D

    更新日期:2004-08-01 00:00:00

  • Functional expression of a cDNA encoding a human ecto-ATPase.

    abstract::1 The metabolism of extracellular nucleotides plays an important role in nucleotide signalling mediated by P2 receptors. The nucleotide sequence encoding a putative human ecto-ATPase named CD39L1 was reported recently. However, the biological activity of this protein has not been established. 2 Based on the sequence o...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702805

    authors: Mateo J,Harden TK,Boyer JL

    更新日期:1999-09-01 00:00:00

  • Feedback inhibition of nitric oxide synthase activity by nitric oxide.

    abstract::1. A murine macrophage cell line, J774, expressed nitric oxide (NO) synthase activity in response to interferon-gamma (IFN-gamma, 10 u ml-1) plus lipopolysaccharide (LPS, 10 ng ml-1). The enzyme activity was first detectable 6 h after incubation, peaked at 12 h and became undetectable after 48 h. 2. The decline in the...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1993.tb12886.x

    authors: Assreuy J,Cunha FQ,Liew FY,Moncada S

    更新日期:1993-03-01 00:00:00

  • Therapeutic potential of NADPH oxidase 1/4 inhibitors.

    abstract::The NADPH oxidase (NOX) family of enzymes produces ROS as their sole function and is becoming recognized as key modulators of signal transduction pathways with a physiological role under acute stress and a pathological role after excessive activation under chronic stress. The seven isoforms differ in their regulation,...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.13532

    authors: Teixeira G,Szyndralewiez C,Molango S,Carnesecchi S,Heitz F,Wiesel P,Wood JM

    更新日期:2017-06-01 00:00:00

  • Pharmacological and certain chemical properties of AH 10407, an unusually short-acting, competitive neuromuscular blocking drug, and some related compounds.

    abstract::1,1-Azobis[3-methyl-2-phenylbenzimidazolinium]dimethanesulphonate (AH 10407) has an ultrashort, competitive neuromuscular blocking action in the mouse, cat, dog, Cynamolgus monkey and cotton-eared marmoset. 2 AH 10407 is chemically unstable in bicarbonate-containing solutions and is degraded to inactive products. The ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1977.tb09738.x

    authors: Brittain RT,Jack D,Tyers MB

    更新日期:1977-09-01 00:00:00

  • The uptake of cardiac glycosides in relation to their actions in isolated cardiac muscle.

    abstract::1. The uptake of (3)H-digitoxin, (3)H-ouabain and (3)H-dihydro-ouabain by isolated guinea-pig atria has been studied and compared with the inhibition of the sodium pump and with the inotropic effect.2. Analysis of the curve relating the uptake of digitoxin and ouabain at equilibrium to the bath concentration enabled a...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1972.tb08146.x

    authors: Godfraind T,Lesne M

    更新日期:1972-11-01 00:00:00

  • The detection of differential beta-adrenoceptor blockade in the cat.

    abstract::1. Tachycardia and bronchodilatation were produced by intravenous dimethylphenylpiperazinium iodide (DMPP) in the spinal or pithed cat. Responses other than those involving beta-adrenoceptors were minimized by appropriate blocking agents.2. With intact adrenals, both the tachycardia and bronchodilatation with 10 mug/k...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1973.tb08256.x

    authors: Parkes MW

    更新日期:1973-08-01 00:00:00

  • Inter-study variability of preclinical in vivo safety studies and translational exposure-QTc relationships--a PKPD meta-analysis.

    abstract:BACKGROUND AND PURPOSE:Preclinical cardiovascular safety studies (CVS) have been compared between facilities with respect to their sensitivity to detect drug-induced QTc prolongation (ΔQTc). Little is known about the consistency of quantitative ΔQTc predictions that are relevant for translation to humans. EXPERIMENTAL...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,meta分析

    doi:10.1111/bph.13218

    authors: Gotta V,Cools F,van Ammel K,Gallacher DJ,Visser SA,Sannajust F,Morissette P,Danhof M,van der Graaf PH

    更新日期:2015-09-01 00:00:00

  • Effect of metformin on glucose metabolism in the splanchnic bed.

    abstract::1. Use of the antihyperglycaemic agent, metformin, is often associated with a small rise in circulating lactate. This study investigates the source of the lactate and examines the effect of metformin on glucose metabolism by the intestine and liver of rats. 2. Changes in plasma glucose and lactate were measured in the...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1992.tb09093.x

    authors: Bailey CJ,Wilcock C,Day C

    更新日期:1992-04-01 00:00:00

  • A comparison of the inhibitory effects of sodium nitroprusside, pinacidil and nifedipine on pressor response to NG-nitro-L-arginine.

    abstract::1. The inhibitory effects of sodium nitroprusside (SNP), a nitric oxide (NO) donor, on mean arterial pressure (MAP) responses to NG-nitro-L-arginine (L-NNA) (NO synthase inhibitor), angiotensin II (AII) and noradrenaline (NA) were compared with those of pinacidil (KATP channel opener) and nifedipine (L-type calcium an...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1993.tb12816.x

    authors: Wang YX,Zhou T,Pang CC

    更新日期:1993-02-01 00:00:00