A reduction of epidermal growth factor receptor is involved in brefelamide-induced inhibition of phosphorylation of ERK in human astrocytoma cells.

Abstract:

:Brefelamide is an aromatic amide isolated from Dictyostelium cellular slime molds. We found that brefelamide has a potent inhibitory growth effect measured by MTT assay in 1321N1 human astrocytoma cells. The inhibition was associated with reduced phosphorylation of extracellular signal-regulated kinase (ERK). Brefelamide inhibited epidermal growth factor (EGF)-induced phosphorylation of ERK in a concentration-dependent manner. Furthermore, brefelamide diminished EGF-induced phosphorylation of EGF receptor at Tyr(1068), a Grb2 binding site that leads to an activation of the Ras/Raf/ERK system. Brefelamide also reduced the expression level of the EGF receptor. These results suggest that one of the mechanisms of action of brefelamide is assumed to be inhibition of phosphorylation of ERK through a reduction of EGF receptor activity in 1321N1 human astrocytoma cells.

journal_name

Eur J Pharmacol

authors

Honma S,Saito M,Kikuchi H,Saito Y,Oshima Y,Nakahata N,Yoshida M

doi

10.1016/j.ejphar.2009.06.030

subject

Has Abstract

pub_date

2009-08-15 00:00:00

pages

38-42

issue

1-3

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(09)00545-7

journal_volume

616

pub_type

杂志文章
  • Different sulfonylurea and ATP sensitivity characterizes the juvenile and the adult form of KATP channel complex of rat skeletal muscle.

    abstract::We have described here the changes of the biophysical and pharmacological properties of the sarcolemmal ATP-sensitive K+ channels (KATP) of rat skeletal muscle fibres, occurring from an early postnatal period (5 days) to adulthood (210 days). The age-dependent changes of the mean current of the KATP channel (channel a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(96)00965-x

    authors: Tricarico D,Petruzzi R,Conte Camerino DC

    更新日期:1997-03-05 00:00:00

  • Vagally mediated reflex and cardiac slowing induced by loperamide in rats.

    abstract::The intravenous injection of loperamide induced an immediate fall in blood pressure and heart rate in anaesthetized rats. Both effects were inhibited by the opiate antagonists naloxone and MRZ 2266 BS. Bilateral vagotomy also inhibited both effects whereas atropine only reduced the bradycardia, but the combination of ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90054-8

    authors: Gautret B,Schmitt H

    更新日期:1985-01-02 00:00:00

  • Cerebroprotective properties of SM-20220, a potent Na(+)/H(+) exchange inhibitor, in transient cerebral ischemia in rats.

    abstract::The aim of this study was to investigate the contribution of the Na(+)/H(+) exchanger to cerebral ischemia using SM-20220 (N-(aminoiminomethyl)-1-methyl-1H-indole-2-carboxamide methanesulfonate), a newly synthesized compound. In in vitro experiments, we evaluated the inhibitory effect of SM-20220 on the Na(+)/H(+) exc...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00645-7

    authors: Kuribayashi Y,Itoh N,Kitano M,Ohashi N

    更新日期:1999-10-27 00:00:00

  • Unique agonist-bound cannabinoid CB1 receptor conformations indicate agonist specificity in signaling.

    abstract::Cannabinoid drugs differ in their rank order of potency to produce analgesia versus other central nervous system effects. We propose that these differences are due to unique agonist-bound cannabinoid CB1 receptor conformations that exhibit different affinities for individual subsets of intracellular signal transductio...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.11.053

    authors: Georgieva T,Devanathan S,Stropova D,Park CK,Salamon Z,Tollin G,Hruby VJ,Roeske WR,Yamamura HI,Varga E

    更新日期:2008-02-26 00:00:00

  • The calcium channel antagonist S 11568 causes endothelium-dependent relaxation in canine arteries.

    abstract::The new dihydropyridine calcium channel antagonist S 11568 and its optical isomers, S 12967 and S 12968 (3 x 10(-6) to 10(-4) M), caused, unlike nifedipine (10(-4) M), equipotent and rapid endothelium-dependent relaxations and increased the content of cyclic GMP in rings of canine femoral arteries. These effects were ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90362-t

    authors: Vilaine JP,Biondi ML,Villeneuve N,Feletou M,Peglion JL,Vanhoutte PM

    更新日期:1991-05-02 00:00:00

  • Exposure to an elevated platform increases plasma corticosterone and hippocampal acetylcholine in the rat: reversal by chlordiazepoxide.

    abstract::There is evidence that the septohippocampal cholinergic system is activated in response to stressful stimuli. In addition, prior studies indicate that stimulating the hippocampal cholinergic neurotransmission increases open arm exploration in the elevated plus-maze. This raises the possibility that exposing the rat to...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.04.011

    authors: Degroot A,Wade M,Salhoff C,Davis RJ,Tzavara ET,Nomikos GG

    更新日期:2004-06-16 00:00:00

  • Possible involvement of S-nitrosylation of brain cyclooxygenase-1 in bombesin-induced central activation of adrenomedullary outflow in rats.

    abstract::We previously reported that both nitric oxide (NO) generated from NO synthase by bombesin and NO generated from SIN-1 (NO donor) activate the brain cyclooxygenase (COX) (COX-1 for bombesin), thereby eliciting the secretion of both catecholamines (CA) from the adrenal medulla by brain thromboxane A(2)-mediated mechanis...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.01.005

    authors: Tanaka K,Shimizu T,Lu L,Yokotani K

    更新日期:2012-03-15 00:00:00

  • Efficacy of the thromboxane receptor antagonist NTP42 alone, or in combination with sildenafil, in the sugen/hypoxia-induced model of pulmonary arterial hypertension.

    abstract::NTP42 is a novel antagonist of the thromboxane A2 receptor (TP) in development for the treatment of pulmonary arterial hypertension (PAH). Recent studies demonstrated that NTP42 and TP antagonism have a role in alleviating PAH pathophysiology. However, the efficacy of NTP42 when used in combination with existing PAH t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173658

    authors: Mulvaney EP,Reid HM,Bialesova L,Mendes-Ferreira P,Adão R,Brás-Silva C,Kinsella BT

    更新日期:2020-12-15 00:00:00

  • Sensitivity of histamine H3 receptor agonist-stimulated [35S]GTP gamma[S] binding to pertussis toxin.

    abstract::The effect of histamine H3 receptor-selective ligands on [35S]guanosine 5'-o-(gamma-thio)triphosphate ([35S]GTP gamma[S]) binding has been examined in rat cerebral cortical membranes. R alpha-Methylhistamine and N alpha-methylhistamine produced a concentration-dependent stimulation of [35S]GTP gamma[S] binding which w...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00800-4

    authors: Clark EA,Hill SJ

    更新日期:1996-01-25 00:00:00

  • Mechanism for resveratrol-induced cardioprotection against reperfusion injury involves glycogen synthase kinase 3beta and mitochondrial permeability transition pore.

    abstract::Resveratrol pretreatment can protect the heart by inducing pharmacological preconditioning. Whether resveratrol protects the heart when applied at reperfusion remains unknown. We examined the effect of resveratrol on myocardial infarct size when given at reperfusion and investigated the mechanism underlying the effect...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.12.024

    authors: Xi J,Wang H,Mueller RA,Norfleet EA,Xu Z

    更新日期:2009-02-14 00:00:00

  • Mast cells, brain inflammation and autism.

    abstract::Increasing evidence indicates that brain inflammation is involved in the pathogenesis of neuropsychiatric diseases. Mast cells (MCs) are located perivascularly close to neurons and microglia, primarily in the leptomeninges, thalamus, hypothalamus and especially the median eminence. Corticotropin-releasing factor (CRF)...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2015.03.086

    authors: Theoharides TC,Stewart JM,Panagiotidou S,Melamed I

    更新日期:2016-05-05 00:00:00

  • Modulation of ischemia-evoked release of excitatory and inhibitory amino acids by adenosine A1 receptor agonist.

    abstract::Adenosine has been reported to have beneficial effects against ischemic brain damage, although the mechanisms are not fully clarified. To examine the role of adenosine on the ischemia-evoked release of neurotransmitters, we applied a highly selective agonist for adenosine A1 receptor, 2-chloro-N6-cyclopentyladenosine ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00559-7

    authors: Goda H,Ooboshi H,Nakane H,Ibayashi S,Sadoshima S,Fujishima M

    更新日期:1998-09-18 00:00:00

  • Prevention of aortic calcification by etidronate in the renal failure rat model.

    abstract::Our recent clinical study indicated that etidronate may inhibit the progression of aortic calcification in hemodialysis patients. To determine whether etidronate inhibits aortic calcification in renal failure rats, renal failure was induced by subtotal nephrectomy, in which 5/6 of the kidneys were removed. Significant...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.12.006

    authors: Tamura K,Suzuki Y,Matsushita M,Fujii H,Miyaura C,Aizawa S,Kogo H

    更新日期:2007-03-08 00:00:00

  • Comparison between dopamine transporter affinity and self-administration potency of local anesthetics in rhesus monkeys.

    abstract::Local anesthetics bind to dopamine transporters and inhibit dopamine uptake in rodent brain. Additionally, local anesthetics are self-administered in rhesus monkeys. The present study determined binding affinities of cocaine and five local anesthetics at dopamine transporters in rhesus monkey brain, and compared bindi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00967-4

    authors: Wilcox KM,Paul IA,Woolverton WL

    更新日期:1999-02-19 00:00:00

  • Anticancer effects and possible mechanisms of lycopene intervention on N-methylbenzylnitrosamine induced esophageal cancer in F344 rats based on PPARγ1.

    abstract::Lycopene, a natural carotenoid, has potential chemopreventive effects in many cancers. This study aimed to examine the effects of lycopene on regulating the inflammation and apoptosis of N-nitrosomethylbenzylamine(NMBzA) induced esophageal cancer in F344 rats. After the rats were fed normal diets containing different ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173230

    authors: Cui L,Xu F,Wu K,Li L,Qiao T,Li Z,Chen T,Sun C

    更新日期:2020-08-15 00:00:00

  • A comparison of the vasodepressor effects of the cyclic effects of the cyclic endoperoxides PGG, and PGH2 with those of PGD2 and PGE2 in hypertensive and normotensive rats.

    abstract::The vasodepressor actions of the cyclic endoperoxides PGG2 and PGH2 were compared with those of their products PGD2 and PGE2 using anaesthetised normotensive and genetically hypertensive rats. Given into the aortic arch of normotensives PGE2 was approximately 6 times more potent than PGH2 and 11 times more potent tha...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(76)90133-3

    authors: Armstrong JM,Boura AL,Hamberg M,Samuelsson B

    更新日期:1976-10-01 00:00:00

  • Increase in renal phorbol ester receptors in rats with cyclosporine A-induced nephrotoxicity.

    abstract::Treatment of rats with cyclosporine A (50 mg/kg i.p.) for 4 days resulted in the impairment of renal function. Renal membrane and soluble phorbol ester receptor densities were significantly higher in cyclosporine A-treated rats compared to vehicle-treated rats. These data suggest that increased phorbol ester receptor ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90396-8

    authors: Nambi P,Pullen M,Wu HL,Brooks DP

    更新日期:1991-03-19 00:00:00

  • Receptor polymorphisms and diseases.

    abstract::The aim of our review is to summarize common genetic variations of some receptors associated with clinical consequences, which were not outlined in the previous special issue of this journal. Because of the multiple pathomechanisms of diseases, a set of genetic variation can play a role in the development of pathologi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/s0014-2999(01)00755-5

    authors: Császár A,Abel T

    更新日期:2001-02-23 00:00:00

  • Nature of functional tolerance produced by chronic flurazepam treatment in the cat.

    abstract::Cats were treated once daily for 35 days with flurazepam (FZP). Different groups received 2, 5 or 20 mg/kg per day. A fourth group was started at 20 mg/kg per day, then the dose was increased to 30, and finally 40 mg/kg per day. Muscle relaxation, ataxia, and other measures of neurological impairment were used to meas...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(82)90100-5

    authors: Rosenberg HC,Chiu TH

    更新日期:1982-07-16 00:00:00

  • Effects of platelet activating factor receptor antagonists on intracellular platelet activating factor function in neutrophils.

    abstract::We investigated the effects of the platelet activating factor (PAF) receptor antagonists, SM-12502 ((+)-cis-3,5-dimethyl-2-(pyridyl)- thiazolidin-4-one hydrochloride), WEB-2086 (3-(4-(2-chlorphenyl)-9-methyl-6H-thieno(3,2-f)-(1,2,4)triazolo(4, 3- a)(1,4)diazepin-2-yl)-1-(4-morpholinyl)-1-propanone) and RP-48740 (3-(3-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(94)90037-x

    authors: Koike H,Imanishi N,Natsume Y,Morooka S

    更新日期:1994-11-15 00:00:00

  • Central monoaminergic mechanisms in mice and analgesic activity of spiradoline mesylate, a selective kappa-opioid receptor agonist.

    abstract::We assessed the roles of brain monoaminergic systems in the analgesic action of spiradoline, a novel kappa-opioid agonist, behaviorally and biochemically by using noradrenaline (NE) and serotonin (5-HT) uptake inhibitors. Analgesic activity was evaluated by measuring latency time in the mouse tail-pinch test. Spiradol...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90107-f

    authors: Kunihara M,Ohyama M,Nakano M

    更新日期:1992-04-22 00:00:00

  • The gut as communicator between environment and host: immunological consequences.

    abstract::During human evolution, the mucosal immune system developed two anti-inflammatory mechanisms: immune exclusion by secretory antibodies (SIgA and SIgM) to control epithelial colonization of microorganisms and inhibit penetration of harmful substances; and immunosuppression to counteract local and peripheral hypersensit...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2011.07.006

    authors: Brandtzaeg P

    更新日期:2011-09-01 00:00:00

  • The mechanism of apoptosis induced by a novel thioredoxin reductase inhibitor in A549 cells: possible involvement of nuclear factor-kappaB-dependent pathway.

    abstract::1,2-[bis(1,2-benzisoselenazolone-3(2H)-ketone)]ethane (BBSKE, PCT: CN02/00412), a novel thioredoxin reductase inhibitor previously synthesized in our lab, has been demonstrated to inhibit the growth of a variety of human cancer cells and to induce apoptosis. Here we report on the potential molecular mechanism of apopt...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.10.037

    authors: Lan L,Zhao F,Wang Y,Zeng H

    更新日期:2007-01-26 00:00:00

  • Interference of the PAF receptor antagonist, PCA 4248, with the rat pleurisy evoked by inflammatory mediators or allergen.

    abstract::This study investigated the effect of the platelet-activating factor (PAF) receptor antagonist, PCA 4248, on the rat pleurisy caused by PAF, serotonin, bradykinin, histamine or allergen. The pleurisy was assessed by measuring liquid extravasation and leucocyte infiltration. Oral pretreatment with PCA 4248 (2.5-20 mg/k...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90087-x

    authors: Martins MA,Lima MC,Bozza PT,Faria Neto HC,Silva PM,Sunkel CE,Cordeiro RS

    更新日期:1993-06-11 00:00:00

  • The effect of chronic administration of caffeine on morphine-induced analgesia, tolerance and dependence in mice.

    abstract::Morphine-induced analgesia, and the development of morphine-induced tolerance and dependence was determined in mice which had drunk caffeinated water (1 mg/ml) for 14 days or in mice which had received (-)-N6-(phenylisopropyl)-adenosine (PIA) 1 mg/kg i.p. for 14 days. Analgesia was assessed by the tail flick assay. Th...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90635-7

    authors: Ahlijanian MK,Takemori AE

    更新日期:1986-01-14 00:00:00

  • Rosuvastatin inhibits norepinephrine-induced cardiac hypertrophy via suppression of Gh.

    abstract::Statins have recently been shown to produce anti-cardiac hypertrophic effects via the regulation of small GTPases. However, the effects of statins on G protein-mediated cardiac hypertrophy, which is the main pathway of cardiac hypertrophy, have not yet been studied. We sought to evaluate whether statin treatment direc...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2009.10.050

    authors: Choi EY,Chang W,Lim S,Song BW,Cha MJ,Kim HJ,Choi E,Jang Y,Chung N,Hwang KC

    更新日期:2010-02-10 00:00:00

  • The many different faces of major depression: it is time for personalized medicine.

    abstract::First line antidepressants are the so-called SSRIs (selective serotonin reuptake inhibitors), e.g. fluvoxamine, fluoxetine, sertraline, paroxetine and escitalopram. Unfortunately, these drugs mostly do not provide full symptom relief and have a slow onset of action. Therefore other antidepressants are also being presc...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2014.11.045

    authors: Korte SM,Prins J,Krajnc AM,Hendriksen H,Oosting RS,Westphal KG,Korte-Bouws GA,Olivier B

    更新日期:2015-04-15 00:00:00

  • Vasopressin V1A receptor mediates cell proliferation through GRK2-EGFR-ERK1/2 pathway in A7r5 cells.

    abstract::Abnormal proliferation and hypertrophy of vascular smooth muscle (VSMC), as the main structural component of the vasculature, is an important pathological mechanism of hypertension. Recently, increased levels of arginine vasopressin (AVP) and copeptin, the C-terminal fragment of provasopressin, have been shown to corr...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.10.023

    authors: Zhang L,Wang X,Cao H,Chen Y,Chen X,Zhao X,Xu F,Wang Y,Woo AY,Zhu W

    更新日期:2016-12-05 00:00:00

  • Oral treatment with probucol in a pharmacological dose has no beneficial effects on mortality in chronic ischemic heart failure after large myocardial infarction in rats.

    abstract::Cardiac remodeling after myocardial infarction is in part triggered and maintained by reactive oxygen species. Antioxidants such as probucol have shown positive short-term effects on these cardiac interstitial changes in different experimental models after intraperitoneal administration or after per-oral administratio...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.11.049

    authors: Betge S,Lutz K,Roskos M,Figulla HR

    更新日期:2007-03-08 00:00:00

  • Function of multidrug resistance-associated protein 2 in acute hepatic failure rats.

    abstract::The function of multidrug resistance-associated protein 2 (Mrp2) in the intestine and liver, as well as intestinal Mrp2 expression, was analyzed in CCl(4)-induced acute hepatic failure rats with hyperbilirubinemia. The plasma level of bilirubin glucuronides, endogenous Mrp2-substrates, was 26 microM at 24 h after CCl(...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.06.079

    authors: Yokooji T,Murakami T,Yumoto R,Nagai J,Takano M

    更新日期:2006-09-28 00:00:00