当前位置： SCI文献检索 > BIOCHEMICAL PHARMACOLOGY期刊下所有文献 > Human adenosine A(3) receptor leads to intracellular Ca(2+) mobilization but is insufficient to activate the signaling pathway via phosphoinositide 3-kinase gamma in mice.

Human adenosine A(3) receptor leads to intracellular Ca(2+) mobilization but is insufficient to activate the signaling pathway via phosphoinositide 3-kinase gamma in mice.

Abstract：

:Selective antagonists for the adenosine A(3) receptor (A3AR), a member of the G protein-coupled receptors, have been indicated as potential drugs for anti-asthma or anti-inflammation. However, potent antagonists for the rodent A3AR have not been identified. To evaluate the pharmacological effects of human A3AR antagonists in mice, we here generated A3AR-humanized mice, in which the mouse A3AR gene was replaced by its human counterpart. The expression levels of human A3AR in the A3AR-humanized mice were equivalent to those of mouse A3AR in wild-type mice. Elevation of the intracellular Ca(2+) concentration induced by an A3AR agonist was observed in bone marrow-derived mast cells from the A3AR-humanized mice and this Ca(2+) mobilization was completely antagonized by a human A3AR antagonist. However, antigen-dependent degranulation was not potentiated by the A3AR agonist in the mast cells from A3AR-humanized mice. The agonist-stimulated human A3AR did not lead to the phosphorylation of either extracellular signal-regulated kinase 1/2 or protein kinase B in A3AR-humanized mice. The rate of human A3AR internalization in the mast cells was also markedly decreased compared with that of mouse A3AR in the mast cells. These results demonstrate that the human A3AR is insufficient to activate phosphoinositide 3-kinase gamma-dependent signaling pathways in mice, probably due to the uncoupling of member(s) of the G proteins, which are capable of activating phosphoinositide 3-kinase gamma, to the human A3AR, despite the mouse G protein(s) responsible for the Ca(2+) elevation are coupled with the human A3AR.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Yamano K,Inoue M,Masaki S,Saki M,Ichimura M,Satoh M

doi

10.1016/j.bcp.2005.08.003

subject

Has Abstract

pub_date

2005-11-15 00:00:00

pages

1487-96

issue

10

eissn

0006-2952

issn

1873-2968

pii

S0006-2952(05)00529-0

journal_volume

70

pub_type

杂志文章

相关文献

BIOCHEMICAL PHARMACOLOGY文献大全
  • Sulfated polymannuroguluronate, a novel anti-AIDS drug candidate, inhibits HIV-1 Tat-induced angiogenesis in Kaposi's sarcoma cells.

    abstract：:Kaposi's sarcoma (KS), a neoplasm often associated with iatrogenic and acquired immunosuppression, is characterized by prominent angiogenesis. Angiogenic factors released from KS and host cells and HIV viral products-the protein Tat are reported to be involved in angiogenesis. Mounting evidence further suggests that m...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2007.06.012

    authors： Lu CX,Li J,Sun YX,Qi X,Wang QJ,Xin XL,Geng MY

    更新日期：2007-11-01 00:00:00

  • Phospholipase A2 activity in carrageenin-induced inflammatory tissue of rats.

    abstract：:Phospholipase A2 activity was detected in 7-day-old carrageenin-induced inflammatory tissue of rats using a synthetic substrate. 1-acyl-2-[3H]arachidonyl-phosphatidylcholine. The inflammatory tissue was homogenized in saline containing 1 M KCl, and the 105,000 g supernatant fraction was placed on a Sephadex G-100 colu...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(82)90275-1

    authors： Ohuchi K,Watanabe M,Numajiri N,Tsurufuji S

    更新日期：1982-09-15 00:00:00

  • Inhibition of human red blood cell glutathione reductase by valproic acid.

    abstract：:Glutathione reductase (GR) one of the enzymes of the glutathione redox cycle, plays a salient role in maintaining appropriate cellular levels of reduced glutathione. The enzyme in human red blood cells is inhibited in vitro by the anticonvulsant drug valproic acid (VPA). The inhibition is dose-dependent, reversible, u...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(92)90559-2

    authors： Cotariu D,Evans S,Lahat E,Theitler J,Bistritzer T,Zaidman JL

    更新日期：1992-02-04 00:00:00

  • Flow linear dichroism supports an accordion model for the salt-induced condensation of chromatin.

    abstract：:The salt-induced condensation of chromatin has been studied with flow-linear dichroism technique using an intercalative dye (methylene blue) to selectively monitor the linker orientation. At low ionic strength both linkers and chromatosomes (with their flat faces) are oriented preferentially parallel to the chromatin ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(88)90459-5

    authors： Kubista M,Nielsen PE,Nordén B

    更新日期：1988-05-01 00:00:00

  • Inhibition of lipopolysaccharide-induced expression of inducible nitric oxide synthase by phenolic (3E)-4-(2-hydroxyphenyl)but-3-en-2-one in RAW 264.7 macrophages.

    abstract：:The large amount of nitric oxide (NO) produced by inducible NO synthase (iNOS) contributes to cellular injury in inflammatory disease. In the present study, a novel synthetic compound (3E)-4-(2-hydroxyphenyl)but-3-en-2-one (HPB) was found to inhibit lipopolysaccharide (LPS)-induced NO generation, but not through the i...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2005.05.032

    authors： Tsao LT,Tsai PS,Lin RH,Huang LJ,Kuo SC,Wang JP

    更新日期：2005-08-15 00:00:00

  • PGE2 receptors in detrusor muscle: Drugging the undruggable for urgency.

    abstract：:Overactive bladder (OAB) syndrome is a prevalent condition of the lower urinary tract that causes symptoms, such as urinary frequency, urinary urgency, urge incontinence, and nocturia, and disproportionately affects women and the elderly. Current medications for OAB merely provide symptomatic relief with considerable ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.bcp.2020.114363

    authors： Hou R,Yu Y,Jiang J

    更新日期：2020-12-09 00:00:00

  • Differential regulation of a fibroblast growth factor-binding protein by receptor-selective analogs of retinoic acid.

    abstract：:We have demonstrated earlier that a secreted fibroblast growth factor-binding protein (FGF-BP) can enhance angiogenesis and promote tumor growth in vivo. Furthermore, we found that FGF-BP expression in squamous cell carcinoma (SCC) is reduced by concentrations of retinoids that are effective in the treatment of SCC an...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(00)00507-4

    authors： Boyle BJ,Harris VK,Liaudet-Coopman ED,Riegel AT,Wellstein A

    更新日期：2000-12-01 00:00:00

  • Subcellular distribution of the antidepressant drug desipramine in cultured human fibroblasts after chronic administration. Drug-effect on the subcellular distribution of accumulated phospholipids.

    abstract：:Desipramine (DMI) is an important antidepressant drug and a lysosomotropic substance. In cultured fibroblasts it interferes with lysosomal functions, e.g. phospholipid degradation. Chronic exposure of cells with DMI induces storage of phospholipids. Subcellular fractionations of cultured human fibroblasts that had bee...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(87)90716-7

    authors： Stoffel P,Burkart T,Honegger UE,Wiesmann UN

    更新日期：1987-03-01 00:00:00

  • Cellular distribution and cellular reactivity of platinum (II) complexes.

    abstract：:We have investigated whether or not the cellular content of reactive platinum, aside from total cellular and DNA-bound platinum, is a measure of the growth inhibitory potential of a given platinum complex. Human MCF-7 breast cancer cells, after treatment with cisplatin [cis-diamminedichloroplatinum(II)] and several 1,...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(96)00106-2

    authors： Lindauer E,Holler E

    更新日期：1996-07-12 00:00:00

  • Suppression of vascular cell adhesion molecule-1 expression by crocetin contributes to attenuation of atherosclerosis in hypercholesterolemic rabbits.

    abstract：:To elucidate the molecular mechanism by which antioxidants alleviate atherosclerosis, we investigated the effect of crocetin, a naturally occurred carotinoid with potent antioxidant power, on vascular cell adhesion molecule-1 (VCAM-1) expression in atherosclerotic rabbits. Twenty-four male New Zealand White rabbits we...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2005.07.034

    authors： Zheng S,Qian Z,Tang F,Sheng L

    更新日期：2005-10-15 00:00:00

  • Modifications of deoxycytidine kinase and deaminase activities by docosahexaenoic acid in normal and transformed rat fibroblasts.

    abstract：:Deoxycytidine kinase (dCK) and deoxycytidine deaminase (dCDA) are two key enzymes in the activation and inactivation, respectively, of deoxycytidine (dCyd) and several chemotherapeutically important nucleoside analogues. To investigate whether supplementation of docosahexaenoic acid, an n-3 fatty acid found mainly in ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(01)00900-5

    authors： Cha MC,Meckling-Gill KA

    更新日期：2002-02-15 00:00:00

  • Heat shock protein 70 protects against bleomycin-induced pulmonary fibrosis in mice.

    abstract：:Idiopathic pulmonary fibrosis (IPF) involves infiltration of leucocytes, pulmonary injury, fibrosis and resulting pulmonary dysfunction. Myofibroblasts and transforming growth factor (TGF)-beta1 have been suggested to play a major role in the pathology and the myofibroblasts are derived from both lung epithelial cells...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2010.05.025

    authors： Tanaka K,Tanaka Y,Namba T,Azuma A,Mizushima T

    更新日期：2010-09-15 00:00:00

  • Formation of mono- and diglucuronides and other glycosides of benzo(a)pyrene-3,6-quinol by V79 cell-expressed human phenol UDP-glucuronosyltransferases of the UGT1 gene complex.

    abstract：:Glucuronidation of quinols of polycyclic aromatic hydrocarbons (PAHs) represents an important detoxication pathway preventing toxic quinone/quinol redox cycles. Therefore, mono- and diglucuronide formation of benzo(a)pyrene-3,6-quinol was investigated and compared to that of structurally related 3,6-dihydroxychrysene ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(95)00095-h

    authors： Gschaidmeier H,Seidel A,Burchell B,Bock KW

    更新日期：1995-05-26 00:00:00

  • Identification of new highly selective inhibitors of the human ADP/ATP carriers by molecular docking and in vitro transport assays.

    abstract：:Mitochondrial carriers are proteins that shuttle a variety of metabolites, nucleotides and coenzymes across the inner mitochondrial membrane. The mitochondrial ADP/ATP carriers (AACs) specifically translocate the ATP synthesized within mitochondria to the cytosol in exchange for the cytosolic ADP, playing a key role i...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2015.11.019

    authors： Todisco S,Di Noia MA,Onofrio A,Parisi G,Punzi G,Redavid G,De Grassi A,Pierri CL

    更新日期：2016-01-15 00:00:00

  • The interaction of oral hypoglycaemic drugs with insulin on steroid metabolism in hepatocytes isolated from control and diabetic male rats.

    abstract：:The effects of the oral hypoglycaemic drugs, phenformin and tolbutamide, and insulin, alone and in combination, on steroid metabolism in hepatocytes isolated from control and streptozotocin-diabetic male rats has been studied. Both phenformin and tolbutamide mimic the action of insulin in stimulating hepatic steroid m...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(90)90724-y

    authors： Hussin AH,Skett P

    更新日期：1990-11-15 00:00:00

  • My close encounter with GABA(B) receptors.

    abstract：:In this review, I summarize the sequence of events involved in characterizing the functional role of GABA(B) receptors in the CNS and their involvement in synaptic transmission. The story was launched with the realization that baclofen was a selective agonist of GABA(B) receptors. This lead to the discovery in the CNS...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.bcp.2004.07.024

    authors： Nicoll RA

    更新日期：2004-10-15 00:00:00

  • Targeting ROCK1/2 blocks cell division and induces mitotic catastrophe in hepatocellular carcinoma.

    abstract：BACKGROUND:Rho-Associated kinases ROCK1 and ROCK2 have been extensively investigated in the pathogenesis of cardiovascular disease. However, their roles are not fully understood in carcinogenesis. In this study, we investigated whether ROCK1 or ROCK2 is required for the survival and growth of hepatocellular carcinoma (...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2020.114353

    authors： Wu H,Chen Y,Li B,Li C,Guo J,You J,Hu X,Kuang D,Qi S,Liu P,Li L,Xu C

    更新日期：2020-12-02 00:00:00

  • Dopamine- and L-beta-3,4-dihydroxyphenylalanine hydrochloride (L-Dopa)-induced cytotoxicity towards catecholaminergic neuroblastoma SH-SY5Y cells. Effects of oxidative stress and antioxidative factors.

    abstract：:Enhanced oxidative stress has been suggested to be involved in the degeneration of nigrostriatal dopaminergic neurons in Parkinson's disease. The high turnover rate of dopamine and/or unsequestered dopamine may cause an increase of formation of hydrogen peroxide via either oxidative deamination of dopamine by monoamin...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(96)00731-9

    authors： Lai CT,Yu PH

    更新日期：1997-02-07 00:00:00

  • Structure-activity relationships of alkylamines that inhibit rat liver hydroxysteroid sulfotransferase activities in vitro.

    abstract：:Tetraalkylammonium salts having n-propyl to n-amyl side chains inhibited rat liver sulfotransferase (ST) activities toward dehydroepiandrosterone and cortisol, but not ST activity toward 2-naphthol, whereas trialkylamines having ethyl to n-amyl side chains inhibited ST activity toward dehydroepiandrosterone, but not S...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(94)00495-8

    authors： Matsui M,Takahashi M,Miwa Y,Motoyoshi Y,Homma H

    更新日期：1995-03-01 00:00:00

  • Induction of human breast cancer cell apoptosis from G2/M preceded by stimulation into the cell cycle by Z-1,1-dichloro-2,3-diphenylcyclopropane.

    abstract：:We have shown previously that Z-1,1-dichloro-2,3-diphenylcyclopropane (a.k.a. Analog II, A(II)) inhibits human breast cancer cell proliferation regardless of estrogen receptor status or estrogen sensitivity, and that its cellular targets include microtubules. In the present study, we investigated the apoptosis-inducin...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(98)00289-5

    authors： Balachandran R,ter Haar E,Yalowich JC,Welsh MJ,Grant SG,Day BW

    更新日期：1999-01-01 00:00:00

  • Participation of active oxygen species in 6-hydroxydopamine toxicity to a human neuroblastoma cell line.

    abstract：:Catalase, superoxide dismutase, and dimethylsulfoxide were tested for their ability to prevent the cytotoxic effect of 6-hydroxydopamine (6-OHDA) on the human neuroblastoma line SY5Y. Viability was measured at two time points after 6-OHDA treatment: at 3 hr by means of amino acid incorporation and at 24 hr by trypan b...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(82)90208-8

    authors： Tiffany-Castiglioni E,Saneto RP,Proctor PH,Perez-Polo JR

    更新日期：1982-01-15 00:00:00

  • Point-to-point ligand-receptor interactions across the subunit interface modulate the induction and stabilization of conformational states of alpha7 nAChR by benzylidene anabaseines.

    abstract：:The homomeric α7 nicotinic acetylcholine receptor is a well-studied therapeutic target, though its characteristically rapid desensitization complicates the development of drugs with specific agonist effects. Moreover, some experimental compounds such as GTS-21 (2,4diMeOBA), a derivative of the α7-selective partial ago...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2013.01.010

    authors： Isaacson MD,Horenstein NA,Stokes C,Kem WR,Papke RL

    更新日期：2013-03-15 00:00:00

  • Growth factors, cytokines and their receptors as downstream targets of arylhydrocarbon receptor (AhR) signaling pathways.

    abstract：:2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) is a widespread environmental pollutant, which causes a variety of severe health effects, e.g. immunosuppression, hepatotoxicity, and carcinogenesis. The main mediator of TCDD toxicity is the arylhydrocarbon receptor (AhR), which, upon activation, translocates into the nucleu...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.bcp.2008.09.013

    authors： Haarmann-Stemmann T,Bothe H,Abel J

    更新日期：2009-02-15 00:00:00

  • gamma-Aminobutyric acid uptake and localization in bovine chromaffin cells in primary culture.

    abstract：:gamma-Aminobutyric acid (GABA) uptake was studied in bovine chromaffin cells maintained in primary culture. Uptake was found to be dependent on Na+, but not on K+ and Ca2+ ions; it was found that 2 Na+ ions were necessary for each molecule of GABA transported. 2,4-Dinitrophenol, ouabain and vanadate inhibited GABA upt...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(89)90459-0

    authors： Oset-Gasque MJ,Aunis D

    更新日期：1989-07-15 00:00:00

  • Role of the CYP2D subfamily in metabolism-dependent covalent binding of propranolol to liver microsomal protein in rats.

    abstract：:In vitro covalent binding of a chemically reactive metabolite of propranolol to microsomal macromolecules, which is presumed to cause inhibition of its own metabolism in rats, was diminished in liver microsomes from rats pretreated with propranolol. Covalent binding was suppressed by the addition of an antibody agains...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(94)90587-8

    authors： Masubuchi Y,Narimatsu S,Hosokawa S,Suzuki T

    更新日期：1994-11-16 00:00:00

  • Desulfuration of 6-mercaptopurine. The basis for the paradoxical cytotoxicity of thiopurines in cultured human leukemic cells.

    abstract：:The thiopurines have a wide array of effects on purine metabolism, but the primary mechanism of cytotoxicity for both 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) appears to be incorporation of drug into DNA following conversion to the thioguanylate form. In murine leukemic cell lines exposed to a range of thiopur...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(93)90333-r

    authors： Adamson PC,Balis FM,Hawkins ME,Murphy RF,Poplack DG

    更新日期：1993-11-02 00:00:00

  • 2-Bromoethylamine as a potent selective suicide inhibitor for semicarbazide-sensitive amine oxidase.

    abstract：:Semicarbazide-sensitive amine oxidase (SSAO) catalyzes the deamination of methylamine and aminoacetone to produce toxic aldehydes, i.e. formaldehyde and methylglyoxal, as well as hydrogen peroxide and ammonia. An increase of SSAO activity was detected by different laboratories in patients suffering from vascular disor...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(01)00524-x

    authors： Yu PH,Davis BA,Deng Y

    更新日期：2001-03-15 00:00:00

  • Decrease in hepatic cytochrome P450 after interleukin-2 immunotherapy.

    abstract：:Interleukin-2 (IL-2) has been shown to decrease cytochrome P450 (CYP) mRNAs and proteins in cultured rat hepatocytes, and IL-2 administration decreases CYPs in rats. Although high doses of IL-2 are administered to cancer patients, the effect on human CYPs has not yet been determined. Patients with hepatic metastases f...

    journal_title：Biochemical pharmacology

    pub_type： 临床试验,杂志文章,随机对照试验

    doi：10.1016/s0006-2952(98)00372-4

    authors： Elkahwaji J,Robin MA,Berson A,Tinel M,Lettéron P,Labbe G,Beaune P,Elias D,Rougier P,Escudier B,Duvillard P,Pessayre D

    更新日期：1999-04-15 00:00:00

  • Activation of acyl-CoA: cholesterol acyltransferase in rat liver microsomes by 25-hydroxycholesterol.

    abstract：:25-Hydroxycholesterol stimulated acyl-CoA:cholesterol acyltransferase (ACAT) activity in rat liver microsomes in vitro with half-maximal stimulation at 16.8 microM oxysterol and a maximal activity that was three times that in its absence. The current study was conducted to determine the effect of 25-hydroxycholesterol...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(96)00649-1

    authors： Bhuvaneswaran C,Synouri-Vrettakou S,Mitropoulos KA

    更新日期：1997-01-10 00:00:00

  • Evidence for distinct regulation processes in the aclacinomycin- and doxorubicin-mediated differentiation of human erythroleukemic cells.

    abstract：:Human erythroleukemic K 562 cells were induced to were induced to differentiate along the erythroid lineage by anthracycline antitumor drugs, such as aclacinomycin (ACLA) and doxorubicin (DOX). Subsequent stimulation of heme and globin synthesis led to a differential quantitative expression of hemoglobins. Gower 1 (ep...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(95)02240-6

    authors： Morceau F,Aries A,Lahlil R,Devy L,Jardillier JC,Jeannesson P,Trentesaux C

    更新日期：1996-03-22 00:00:00