History of the G protein-coupled receptor (GPCR) assays from traditional to a state-of-the-art biosensor assay.

Abstract:

:The G protein-coupled receptors (GPCRs) form the largest and the most versatile superfamily that share a seven-transmembrane-spanning architecture. GPCR-signaling is involved in vision, taste, olfaction, sympathetic/parasympathetic nervous functions, metabolism, and immune regulation, indicating that GPCRs are extremely important therapeutic targets for various diseases. Cellular dielectric spectroscopy (CDS) is a novel technology that employs a label-free, real-time and cell-based assay approach for the comprehensive pharmacological evaluation of cells that exogenously or endogenously express GPCRs. Among the biosensors that use CDS technology, the CellKey™ system not only detects the activation of GPCRs but also distinguishes between signals through different subtypes of the Gα protein (Gs, Gi/o, and Gq). In this review, we discuss the traditional assays and then introduce the principles by which the CellKey™ system evaluates GPCR activation, followed by a perspective on the advantages and future prospects of this system.

journal_name

J Pharmacol Sci

authors

Miyano K,Sudo Y,Yokoyama A,Hisaoka-Nakashima K,Morioka N,Takebayashi M,Nakata Y,Higami Y,Uezono Y

doi

10.1254/jphs.14R13CP

subject

Has Abstract

pub_date

2014-01-01 00:00:00

pages

302-9

issue

4

eissn

1347-8613

issn

1347-8648

pii

DN/JST.JSTAGE/jphs/14R13CP

journal_volume

126

pub_type

杂志文章,评审
  • Schisandra chinensis acidic polysaccharide partialy reverses acetaminophen-induced liver injury in mice.

    abstract::Schisandra chinensis is a hepatoprotective herb that has been used for centuries in China. Polysaccharide is one of the major active components in S. chinensis, which has been reported to improve liver injuries induced by carbon tetrachloride, alcohol, or high-fat diet. In this study, we observed the effects and corre...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2019.07.008

    authors: Che J,Yang S,Qiao Z,Li H,Sun J,Zhuang W,Chen J,Wang C

    更新日期:2019-07-01 00:00:00

  • Roxatidine- and cimetidine-induced angiogenesis inhibition suppresses growth of colon cancer implants in syngeneic mice.

    abstract::Cimetidine is known to suppress the growth of several tumors, including gastrointestinal cancer, in humans and animals. Nonetheless, whether other histamine H(2)-receptor antagonists exert such tumor suppressive effects remains unclear. The effect of roxatidine acetate hydrochloride (roxatidine), an H(2)-receptor anta...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.93.321

    authors: Tomita K,Izumi K,Okabe S

    更新日期:2003-11-01 00:00:00

  • Microminipig, a non-rodent experimental animal optimized for life science research:novel atherosclerosis model induced by high fat and cholesterol diet.

    abstract::Atherosclerotic lesions were observed in male and ovariectomized female Microminipig (MMP) fed a high fat and cholesterol diet with sodium cholate (HFCD/SC) for 3 months. HFCD/SC induced hypercholesterolemia accompanied by an increase in serum total cholesterol (T-Cho), low-density lipoprotein cholesterol (LDL-C), hig...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1254/jphs.10r17fm

    authors: Kawaguchi H,Miyoshi N,Miura N,Fujiki M,Horiuchi M,Izumi Y,Miyajima H,Nagata R,Misumi K,Takeuchi T,Tanimoto A,Yoshida H

    更新日期:2011-01-01 00:00:00

  • Modifications of capsaicin-sensitive neurons in isolated guinea pig ileum by [6]-gingerol and lafutidine.

    abstract::A segment of guinea pig ileum was used to confirm the hypothesis that [6]-gingerol and lafutidine interact with capsaicin-sensitive neurons. Addition of 30 and 100 microM [6]-gingerol (a pungent constituent of ginger) induced contraction of the ileum immediately. Like capsaicin, [6]-gingerol-induced contraction was in...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.92.359

    authors: Someya A,Horie S,Yamamoto H,Murayama T

    更新日期:2003-08-01 00:00:00

  • A receptor-independent effect of estrone sulfate on the HERG channel.

    abstract::We recently reported that physiological concentrations of 17beta-estradiol partially down-regulate cardiac rapidly-activating delayed rectifier K(+) currents (hERG currents) independently of estrogen-receptor signaling. To determine if other estrogens have the same effect as that of 17beta-estradiol, we investigated r...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.08257sc

    authors: Kakusaka S,Asayama M,Kaihara A,Sasano T,Suzuki T,Kurokawa J,Furukawa T

    更新日期:2009-01-01 00:00:00

  • Screening for control genes in mouse hippocampus after transient forebrain ischemia using high-density oligonucleotide array.

    abstract::In conventional relative gene expression analysis (Northern blotting, RT-PCR, and in situ hybridization), housekeeping genes such as the glyceraldehyde-3-phosphate dehydrogenase (GAPDH) and beta-actin genes, whose expression levels are considered stable, have been used as control genes for normalization of RNA quantit...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.fp0050881

    authors: Nishida Y,Sugahara-Kobayashi M,Takahashi Y,Nagata T,Ishikawa K,Asai S

    更新日期:2006-05-01 00:00:00

  • A novel AMPK activator improves hepatic lipid metabolism and leukocyte trafficking in experimental hepatic steatosis.

    abstract::A novel AMP-activated protein kinase (AMPK) activator, IMM-H007 (H007), has been reported to reduce serum lipid levels and inhibit lipid accumulation in the liver in hyperlipidemic animal models. However, how H007 ameliorates hepatic steatosis and inflammation remains unknown. In the present study, H007, at 200 mg/kg,...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2019.05.008

    authors: Peng X,Li J,Wang M,Qu K,Zhu H

    更新日期:2019-06-01 00:00:00

  • Effects of propofol on electrocardiogram measures in mice.

    abstract::We investigated the anesthetic effects of propofol on the electrocardiogram (ECG) in mice. We also compared the effects of isoflurane (2%) inhalation anesthesia, intraperitoneal propofol (50 or 100 mg/kg), and pentobarbital (50 mg/kg) on ECG in mice. Isoflurane inhalation and pentobarbital anesthesia were both associa...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.14181FP

    authors: Shintaku T,Ohba T,Niwa H,Kushikata T,Hirota K,Ono K,Matsuzaki Y,Imaizumi T,Kuwasako K,Sawamura D,Murakami M

    更新日期:2014-01-01 00:00:00

  • Dopamine inhibits lipopolysaccharide-induced nitric oxide production through the formation of dopamine quinone in murine microglia BV-2 cells.

    abstract::Dopamine (DA) has been suggested to modulate functions of glial cells including microglial cells. To reveal the regulatory role of DA in microglial function, in the present study, we investigated the effect of DA on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in murine microglial cell line BV-2. Pret...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2015.11.002

    authors: Yoshioka Y,Sugino Y,Tozawa A,Yamamuro A,Kasai A,Ishimaru Y,Maeda S

    更新日期:2016-02-01 00:00:00

  • Influence of genetic polymorphisms and habitual caffeine intake on the changes in blood pressure, pulse rate, and calculation speed after caffeine intake: A prospective, double blind, randomized trial in healthy volunteers.

    abstract::The aim of this study was to investigate the contribution of gene polymorphisms, in combination with habitual caffeine consumption, to the effect of caffeine intake on hemodynamic and psychoactive parameters. A double-blind, prospective study was conducted with 201 healthy volunteers randomly allocated 2:1 to the caff...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章,随机对照试验

    doi:10.1016/j.jphs.2019.01.006

    authors: Yoshihara T,Zaitsu M,Shiraishi F,Arima H,Takahashi-Yanaga F,Arioka M,Kajioka S,Sasaguri T

    更新日期:2019-03-01 00:00:00

  • Bcl-2 family proteins were involved in pseudolaric acid B-induced autophagy in murine fibrosarcoma L929 cells.

    abstract::Pseudolaric acid B (PAB) exerted cytostatic activity on murine fibrosarcoma L929 cells. The cytostatic mechanism of PAB on L929 cells was investigated in this paper. At 36 h, after 80 microM PAB treatment, the inhibitory ratio was 65.37 +/- 4.12%, and the MDC staining ratio was strongest in L929 cells. 3-Methyladenine...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.08091fp

    authors: Yu J,Li X,Tashiro S,Onodera S,Ikejima T

    更新日期:2008-07-01 00:00:00

  • Neurotoxin A2NTX Blocks Fast Inhibitory and Excitatory Transmitter Release From Presynaptic Terminals.

    abstract::Our recent study showed a possibility that newly developed A2 type botulinum toxin (A2NTX) inhibits both spontaneous and evoked transmitter release from inhibitory (glycinergic or GABAergic) and excitatory (glutamatergic) nerve terminals using rat spinal sacral dorsal commissural nucleus neurons. In the present study,...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.11124FP

    authors: Yamaga T,Aou S,Shin MC,Wakita M,Akaike N

    更新日期:2012-01-01 00:00:00

  • Antivasospastic effects of hydroxyfasudil, a Rho-kinase inhibitor, after subarachnoid hemorrhage.

    abstract::We investigated the anti-vasospastic potential of fasudil's active metabolite, hydroxyfasudil, a Rho-kinase inhibitor, after subarachnoid hemorrhage (SAH) and also its effect on hemorheological abnormalities following cerebral ischemia. Chronic cerebral vasospasm was produced using a two-hemorrhage canine model. On da...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.11075fp

    authors: Satoh S,Takayasu M,Kawasaki K,Ikegaki I,Hitomi A,Yano K,Shibuya M,Asano T

    更新日期:2012-01-01 00:00:00

  • Sargassum hemiphyllum inhibits atopic allergic reaction via the regulation of inflammatory mediators.

    abstract::Sargassum hemiphyllum (SH) has long been used in Korean folk medicine for the therapeutic treatment of various allergic diseases. The effects of SH in previous experimental models, however, have been inconclusive. We studied the effects of methanol extract of SH on mast cells. Our experiments showed that SH significan...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.fp0040326

    authors: Na HJ,Moon PD,Ko SG,Lee HJ,Jung HA,Hong SH,Seo Y,Oh JM,Lee BH,Choi BW,Kim HM

    更新日期:2005-02-01 00:00:00

  • Combined effects of psychostimulants and morphine on locomotor activity in mice.

    abstract::Simultaneous administration of psychostimulants and opioids is a major drug abuse problem worldwide. This combination appears to produce synergistic effects on behavior at low doses; however, there is little direct evidence that the combination is stronger than either drug alone. Therefore, we investigated interaction...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.fpj04039x

    authors: Mori T,Ito S,Narita M,Suzuki T,Sawaguchi T

    更新日期:2004-12-01 00:00:00

  • p38 mitogen-activated protein kinase contributes to angiotensin II-stimulated migration of rat aortic smooth muscle cells.

    abstract::In this study, we clarified the intracellular mechanism of angiotensin II (Ang II) in promoting migration in rat aortic smooth muscle cells (RASMCs). RASMC migration was measured with the Boyden chamber assay, and the result was confirmed with an aortic sprout assay. The activities of kinases were investigated by west...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.fp0070770

    authors: Lee HM,Lee CK,Lee SH,Roh HY,Bae YM,Lee KY,Lim J,Park PJ,Park TK,Lee YL,Won KJ,Kim B

    更新日期:2007-09-01 00:00:00

  • Potent antidiabetic effects of rivoglitazone, a novel peroxisome proliferator-activated receptor-gamma agonist, in obese diabetic rodent models.

    abstract::The pharmacological effects of rivoglitazone, a novel thiazolidinedione-derivative peroxisome proliferator-activated receptor (PPAR)-gamma agonist, were characterized in vitro and in vivo. Rivoglitazone activated human PPARgamma more potently compared with rosiglitazone and pioglitazone and had little effect on PPARal...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.09084fp

    authors: Kanda S,Nakashima R,Takahashi K,Tanaka J,Ogawa J,Ogata T,Yachi M,Araki K,Ohsumi J

    更新日期:2009-10-01 00:00:00

  • The role of nitric oxide in small intestine differs between a single and a consecutive administration of methotrexate to rats.

    abstract::The role of nitric oxide (NO) on intestinal mucosal injury induced by single or consecutive administration of methotrexate was investigated in a rodent model. Rats received methotrexate intraperitoneally either as a single administration (50 mg/kg) or as a consecutive administration (12.5 mg/kg/day) for 4 days. NG-nit...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2020.02.006

    authors: Shiga S,Machida T,Yanada T,Machida M,Hirafuji M,Iizuka K

    更新日期:2020-05-01 00:00:00

  • Vanadate activates Rho A translocation in association with contracting effects in ileal longitudinal smooth muscle of guinea pig.

    abstract::We characterized the effects of vanadate, an inhibitor of tyrosine phosphatase, on the tension, the level of myosin light chain (MLC) phosphorylation, and Rho A activation in intact ileal longitudinal smooth muscle of the guinea pig to study the role of tyrosine phosphorylation in contraction signaling. Vanadate exert...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.fp0030576

    authors: Mori M,Tsushima H

    更新日期:2004-08-01 00:00:00

  • Anti-diabetic effect and mechanism of Kursi Wufarikun Ziyabit in L6 rat skeletal muscle cells.

    abstract::Kursi Wufarikun Ziyabit (KWZ) is a traditional prescription that used in folk tea drinking for its health care effect in treatment of type 2 diabetes mellitus (T2DM) in central Asia. However, the underlying mechanism of KWZ in T2DM has not been investigated extensively. This study designed to observe the effect of KWZ...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2018.06.011

    authors: Edirs S,Jiang L,Xin X,Aisa HA

    更新日期:2018-06-01 00:00:00

  • Role of neurosteroid allopregnanolone on age-related differences in exercise-induced hypoalgesia in rats.

    abstract::The beneficial effects of physical activity for pain are denominated exercise-induced hypoalgesia (EIH). Here, we examined the age-related change and potential role of the neurosteroid allopregnanolone (ALLO) on EIH in rats. Adult and aged rats were randomly divided into one of three groups; non-exercise control, Low-...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2018.11.009

    authors: Aoyama B,Kawano T,Iwata H,Nishigaki A,Yamanaka D,Tateiwa H,Shigematsu-Locatelli M,Eguchi S,Locatelli FM,Yokoyama M

    更新日期:2019-02-01 00:00:00

  • Differential coupling of human endothelin type A receptor to G(q/11) and G(12) proteins: the functional significance of receptor expression level in generating multiple receptor signaling.

    abstract::This study examines the influence of receptor expression level on signaling pathways activated via endothelin type A receptor (ET(A)R) expressed in Chinese hamster ovary cells at 32,100 (ET(A)R-high-CHO) and 893 (ET(A)R-low-CHO) fmolmg protein(-1). Endothelin-1 (ET-1) elicited a sustained increase in intracellular Ca(...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.09233fp

    authors: Horinouchi T,Asano H,Higa T,Nishimoto A,Nishiya T,Muramatsu I,Miwa S

    更新日期:2009-12-01 00:00:00

  • Transcriptional regulation of neuronal genes and its effect on neural functions: gene expression in response to static magnetism in cultured rat hippocampal neurons.

    abstract::We have previously shown a marked but transient increase in DNA binding of the nuclear transcription factor activator protein-1 after brief exposure to static magnetic fields in cultured rat hippocampal neurons, suggesting that exposure to static magnetism would lead to long-term consolidation as well as amplification...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1254/jphs.fmj05001x5

    authors: Hirai T,Yoneda Y

    更新日期:2005-07-01 00:00:00

  • Noninvasive metabolic syndrome model using an extremely small minipig, the microminipig.

    abstract::Metabolic syndrome (MetS) induces serious complications; therefore, we developed a noninvasive MetS model using an extremely small minipig, the Microminipig. For 8 weeks, Microminipigs were administrated a high-fat and high-cholesterol diet (HFCD) for atherosclerosis and N(G)-nitro-l-arginine methyl ester (l-NAME) for...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.14171sc

    authors: Yamaguchi T,Yamazaki T,Kawaguchi H,Tawa M,Nakamura Y,Shiota M,Osada-Oka M,Tanimoto A,Okamura T,Miura K,Iwao H,Yoshiyama M,Izumi Y

    更新日期:2014-01-01 00:00:00

  • Effects of metformin on proliferation and apoptosis of human megakaryoblastic Dami and MEG-01 cells.

    abstract::Metformin has received increasing attention for its potential anticancer activity against certain human leukemia cells, but its effects on human megakaryoblastic cells are unclear. This study aimed to investigate the effects of metformin on proliferation and apoptosis of human megakaryoblastic cells (Dami and MEG-01) ...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.jphs.2017.08.003

    authors: Liang X,Kong P,Wang J,Xu Y,Gao C,Guo G

    更新日期:2017-09-01 00:00:00

  • Hemostatic action of OC-108, a novel agent for hemorrhoids, is associated with regional blood flow arrest induced by acute inflammation.

    abstract::Clinically, hemorrhoidal bleeding and prolapse disappeared immediately after injection of the sclerosing agent OC-108 into submucosa of hemorrhoids. The aim of this study was to elucidate the mechanism of action responsible for the immediate hemostatic effect of OC-108 using anesthetized rats. Subcutaneous injection o...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.fp0060583

    authors: Ono T,Nakagawa H,Fukunari A,Hashimoto T,Komatsu H

    更新日期:2006-11-01 00:00:00

  • Mithramycin, an agent for developing new therapeutic drugs for neurodegenerative diseases.

    abstract::Mithramycin A (MTM) has been shown to inhibit cancer growth by blocking the binding of Sp-family transcription factors to gene regulatory elements and is used for the treatment of leukemia and testicular cancer in the United States. In contrast, MTM has also been shown to exert neuroprotective effects in normal cells....

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1254/jphs.13r02cp

    authors: Osada N,Kosuge Y,Ishige K,Ito Y

    更新日期:2013-01-01 00:00:00

  • Pharmacology in health foods: effects of arachidonic acid and docosahexaenoic acid on the age-related decline in brain and cardiovascular system function.

    abstract::Arachidonic acid (ARA) and docosahexaenoic acid (DHA) are major constituents of cell membranes and play important roles in preserving physiological and psychological function. Recently, data from several studies have indicated that impairments in long-term potentiation (LTP), the process underlying plasticity in synap...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1254/jphs.10r39fm

    authors: Kiso Y

    更新日期:2011-01-01 00:00:00

  • Trans-resveratrol inhibits early blood vessel formation (vasculogenesis) without impairment of embryonic growth.

    abstract::Resveratrol is a stilbene compound found in grapes and other sources. In this study we examined the effects of trans-resveratrol (4.38 - 438 microM/implant) in the vasculogenesis of yolk-sac membranes and its capacity to improve chick embryo growth. High concentrations of the stilbene (43.8 - 438 microM) significantly...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章

    doi:10.1254/jphs.fp0071876

    authors: Dias PF,Berti FV,Siqueira JM Jr,Maraschin M,Gagliardi AR,Ribeiro-do-Valle RM

    更新日期:2008-06-01 00:00:00

  • Nuclear receptors as targets for drug development: crosstalk between peroxisome proliferator-activated receptor gamma and cytokines in bone marrow-derived mesenchymal stem cells.

    abstract::Peroxisome proliferator-activated receptor gamma (PPARgamma) is a ligand-dependent nuclear receptor and regulates adipogenesis and fat metabolism. PPARgamma is activated by fatty acid derivatives and some synthetic compounds such as the thiazolidinediones. In addition, certain cytokines were known to affect the transa...

    journal_title:Journal of pharmacological sciences

    pub_type: 杂志文章,收录出版,评审

    doi:10.1254/jphs.fmj04008x5

    authors: Takada I,Suzawa M,Kato S

    更新日期:2005-02-01 00:00:00