Pharmacological characterization of a selective agonist for bombesin receptor subtype-3.

Abstract:

:Bombesin receptor subtype-3 (BRS-3) is an orphan G protein-coupled receptor in the bombesin receptor family that still awaits identification of its natural ligand. BRS-3 deficient mice develop a mild late-onset obesity with metabolic defects, implicating BRS-3 plays a role in feeding and metabolism. We describe here the pharmacological characterization of a synthetic compound, 16a, which serves as a potent agonist for BRS-3. This compound is selective for BRS-3 as it does not activate neuromedin B or gastrin-releasing peptide receptors, two most closely related bombesin receptors, as well as a series of other GPCRs. We assessed the receptor trafficking of BRS-3 and found that compound 16a promoted beta-arrestin translocation to the cell membrane. Neither central nor peripheral administration of compound 16a affects locomotor activity in mice. Therefore compound 16a is a potential tool to study the function of the BRS-3 system in vitro and possibly in vivo.

authors

Zhang L,Nothacker HP,Wang Z,Bohn LM,Civelli O

doi

10.1016/j.bbrc.2009.07.006

subject

Has Abstract

pub_date

2009-09-18 00:00:00

pages

283-8

issue

2

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(09)01325-4

journal_volume

387

pub_type

杂志文章
  • Vitamin D fails to prevent serum starvation- or staurosporine-induced apoptosis in human and rat osteosarcoma-derived cell lines.

    abstract::Previous studies have suggested that 1,25(OH)2D3, the active form of vitamin D3, may increase the survival of bone-forming osteoblasts through an inhibition of apoptosis. On the other hand, vitamin D3 has also been shown to trigger apoptosis in human cancer cells, including osteosarcoma-derived cell lines. In the pres...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2005.03.061

    authors: Witasp E,Gustafsson AC,Cotgreave I,Lind M,Fadeel B

    更新日期:2005-05-13 00:00:00

  • 2'-Amino-2'-deoxyguanosine is a cofactor for self-splicing in group I catalytic RNA.

    abstract::In investigations on self-splicing in the group I intron of the pre-mRNA from the nrdB gene of bacteriophage T4 it was found that 2'-amino-2'-deoxyguanosine can replace guanosine as cofactor. This is the first guanosine-analogue with a modification in the 2'-position and substantial activity in a group I self-splicing...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/0006-291x(92)90560-8

    authors: Strömberg R,Hahne S,Sjögren AS,Sjöberg BM

    更新日期:1992-03-16 00:00:00

  • The protective effect of orally administered redox nanoparticle on intestinal ischemia-reperfusion injury in mice.

    abstract:BACKGROUND:Intestinal ischemia-reperfusion (I-R) injury is a serious abdominal condition leading to multiple organ failure with high mortality. However, no reliable treatment is available. A redox nanoparticle (RNPO) was recently developed, and its efficacy for several intestinal inflammatory conditions has been report...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2017.11.204

    authors: Ueda T,Takagi T,Katada K,Iida T,Mizushima K,Dohi O,Okayama T,Yoshida N,Kamada K,Uchiyama K,Handa O,Ishikawa T,Konishi H,Naito Y,Nagasaki Y,Itoh Y

    更新日期:2018-01-08 00:00:00

  • Relationship between the G protein signaling and homologous desensitization of G protein-coupled receptors.

    abstract::Signaling and desensitization of G protein-coupled receptor are intimately related, and measuring them separately requires certain parameters that represent desensitization independently of signaling. In this study, we tested whether desensitization requires signaling in three different receptors, beta2-adrenergic rec...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2005.11.070

    authors: Barak LS,Gilchrist J,Becker JM,Kim KM

    更新日期:2006-01-13 00:00:00

  • Bradykinin-induced generation of inositol 1,4,5-trisphosphate in fibroblasts and neuroblastoma cells: effect of pertussis toxin, extracellular calcium, and down-regulation of protein kinase C.

    abstract::The net content of inositol 1,4,5-trisphosphate [Ins(1,4,5)P3] was measured in bradykinin (BK)-stimulated NIH3T3 fibroblasts and neuroblastoma-glioma hybrid cells (NG108-15). BK-mediated production of Ins(1,4,5)P3 was not affected by replacing the medium with Ca2+-free medium, but addition of EGTA (1mM) to Ca2+-free m...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/s0006-291x(88)81035-0

    authors: Fu T,Okano Y,Nozawa Y

    更新日期:1988-12-30 00:00:00

  • Cloning and sequence analysis of a cDNA encoding tetrameric carbonyl reductase of pig lung.

    abstract::A cDNA for tetrameric carbonyl reductase was cloned from a pig lung cDNA library. The cDNA had an open reading frame encoding a protein of 244 amino acid residues with a predicted monomer molecular weight of 25,985. The authenticity of the cDNA was confirmed by a perfect match of 80 amino acids determined from sequenc...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.1993.1967

    authors: Nakanishi M,Deyashiki Y,Nakayama T,Sato K,Hara A

    更新日期:1993-08-16 00:00:00

  • Retroviral suicide vector does not inhibit neointimal growth in a porcine coronary model of restenosis.

    abstract::We attempted to attenuate neointimal formation following vascular injury using a retroviral suicide vector. Epicardial coronary arteries of adult miniature swine were injured by deployment of oversized tantalum stents. One week later, injured segments were exposed to packaged retroviral constructs with or without the ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.1995.1157

    authors: Barbee RW,Stapleton DD,Madras DE,Ré RN,Murgo JP,Davenport WD,Giardina J,Cook JL

    更新日期:1995-02-06 00:00:00

  • Mineralocorticoid receptor-mediated signaling regulates the ion gated sodium channel in vascular endothelial cells and requires an intact cytoskeleton.

    abstract::The PCR analysis followed by sequence alignment showed that both the mineralocorticoid receptor (MCR) and the epithelial sodium channel (ENaC) genes were expressed in the human vascular endothelial cell line (ECV). The growth and multiplication of the ECV in culture were influenced by both aldosterone and the MCR-spec...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.2001.4275

    authors: Golestaneh N,Klein C,Valamanesh F,Suarez G,Agarwal MK,Mirshahi M

    更新日期:2001-02-09 00:00:00

  • TT virus is distributed in various leukocyte subpopulations at distinct levels, with the highest viral load in granulocytes.

    abstract::When TT virus (TTV) DNA was quantitated in whole blood and plasma aliquots from 27 viremic individuals by real-time detection PCR that can detect essentially all TTV genotypes, the TTV load was 6.9 +/- 3.5 (mean +/- standard deviation)-fold higher in the whole blood than in the plasma samples [P < 0.002 (paired t test...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.2001.6183

    authors: Takahashi M,Asabe S,Gotanda Y,Kishimoto J,Tsuda F,Okamoto H

    更新日期:2002-01-11 00:00:00

  • Trafficking of astrocytic vesicles in hippocampal slices.

    abstract::The increasingly appreciated role of astrocytes in neurophysiology dictates a thorough understanding of the mechanisms underlying the communication between astrocytes and neurons. In particular, the uptake and release of signaling substances into/from astrocytes is considered as crucial. The release of different gliot...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2009.10.119

    authors: Potokar M,Kreft M,Lee SY,Takano H,Haydon PG,Zorec R

    更新日期:2009-12-25 00:00:00

  • In vitro demonstration by the rate assay of the presence of small pore in the outer membrane of Pseudomonas aeruginosa.

    abstract::Determination of the rates of saccharide diffusions by the proteoliposomes showed that the outer membrane of Pseudomonas aeruginosa only possesses small diffusion pores and that protein F might have not been involved in the pore formation. Proteoliposomes containing stachyose or Dextan T-10 showed the same relative di...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/s0006-291x(88)80865-9

    authors: Yoshihara E,Gotoh N,Nakae T

    更新日期:1988-10-14 00:00:00

  • Transposon-independent increase of transcription by the Sleeping Beauty transposase.

    abstract::When a plasmid encoding the Sleeping Beauty (SB) transposase (pCMV-SB) was cointroduced with luciferase expression plasmid DNA into mouse skeletal muscle at a molar ratio of 4:1, luciferase gene expression was 5 times higher than the expression without pCMV-SB on day 28. This enhancement was not dependent on the prese...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2004.03.116

    authors: Masuda K,Yamamoto S,Endoh M,Kaneda Y

    更新日期:2004-05-07 00:00:00

  • Studies on the relationship between cell proliferation and cell death: opposite patterns of SGP-2 and ornithine decarboxylase mRNA accumulation in PHA-stimulated human lymphocytes.

    abstract::To assess the relationship between cell proliferation and cell death, the mRNA accumulation of ornithine decarboxylase (ODC) and sulfated glycoprotein 2 (SGP-2) were measured in human peripheral blood lymphocytes (HPBL) 2-6 hours after stimulation with phytohemagglutinin (PHA). ODC is the rate limiting enzyme of polya...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/s0006-291x(05)81254-9

    authors: Grassilli E,Bettuzzi S,Monti D,Ingletti MC,Franceschi C,Corti A

    更新日期:1991-10-15 00:00:00

  • Analysis of gene expression in single human oocytes and preimplantation embryos.

    abstract::Little is known about the gene expression in human oocytes and early embryo development because of the rare availability of the materials. The recent advancement of biotechnology has allowed one to analyze the gene expression in single human oocytes and preimplantation embryos. Gene expression of human lactate dehydro...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2005.11.149

    authors: Li SS,Liu YH,Tseng CN,Singh S

    更新日期:2006-02-03 00:00:00

  • A novel firefly luciferase biosensor enhances the detection of apoptosis induced by ESAT-6 family proteins of Mycobacterium tuberculosis.

    abstract::The activation of caspase-3 is a key surrogate marker for detecting apoptosis. To quantitate caspase-3 activity, we constructed a biosensor comprising a recombinant firefly luciferase containing a caspase-3 cleavage site. When apoptosis was induced, caspase-3 cleavage of the biosensor activated firefly luciferase by a...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2014.09.047

    authors: Shi J,Zhang H,Fang L,Xi Y,Zhou Y,Luo R,Wang D,Xiao S,Chen H

    更新日期:2014-10-03 00:00:00

  • Peroxynitrite-mediated oxidation of ferrous carbonylated myoglobin is limited by carbon monoxide dissociation.

    abstract::Peroxynitrite-mediated oxidation of ferrous nitrosylated myoglobin (Mb(II)-NO) involves the transient ferric nitrosylated species (Mb(III)-NO), followed by ()NO dissociation and formation of ferric myoglobin (Mb(III)). In contrast, peroxynitrite-mediated oxidation of ferrous oxygenated myoglobin (Mb(II)-O2) involves t...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2007.09.053

    authors: Ascenzi P,Ciaccio C,Coletta M

    更新日期:2007-11-30 00:00:00

  • Molecular cloning and characterization of Cup a 4, a new allergen from Cupressus arizonica.

    abstract::Sensitization to Cupressaceae pollen has become one of the most important causes of pollinosis in Western countries during winter and early spring. However, the characterization of the extracts, the allergens involved and the cross-reactivity with other pollen sources still remain poorly studied; in the case of Cupres...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2010.09.079

    authors: Pico de Coaña Y,Parody N,Fuertes MÁ,Carnés J,Roncarolo D,Ariano R,Sastre J,Mistrello G,Alonso C

    更新日期:2010-10-22 00:00:00

  • Reduced secretion and expression of gelatinase profile in Toxoplasma gondii-infected human monocytic cells.

    abstract::The apicomplexan Toxoplasma gondii, an obligate intracellular parasite, can infect humans and a wide range of vertebrates. Following oral infection, the parasite invades tissues by crossing non-permissive biological barriers such as the placenta or the blood-brain barrier. But the molecular mechanisms underlying migra...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2007.05.089

    authors: Buache E,Garnotel R,Aubert D,Gillery P,Villena I

    更新日期:2007-07-27 00:00:00

  • Proteoglycan gene expression in rat liver after partial hepatectomy.

    abstract::Liver regeneration is regulated by several factors. Among these extracellular matrix plays a crucial role in the restoration of normal structure. Proteoglycans are major components of extracellular matrix and they are able to bind growth factors implicated in liver growth. We studied syndecan, perlecan, fibroglycan, a...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.1996.1718

    authors: Gallai M,Sebestyén A,Nagy P,Kovalszky I,Onody T,Thorgeirsson SS

    更新日期:1996-11-21 00:00:00

  • Exercise-induced increase in IL-6 level enhances GLUT4 expression and insulin sensitivity in mouse skeletal muscle.

    abstract::A single bout of exercise is known to increase the insulin sensitivity of skeletal muscle; however, the underlying mechanism of this phenomenon is not fully understood. Because a single bout of exercise induces a transient increase in blood interleukin-6 (IL-6) level, we hypothesized that the enhancement of insulin se...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2016.03.159

    authors: Ikeda SI,Tamura Y,Kakehi S,Sanada H,Kawamori R,Watada H

    更新日期:2016-05-13 00:00:00

  • Inhibitory effect of porphyrins on the proliferation of mouse spleen lymphocytes in vitro.

    abstract::The influence of various porphyrins (deuteroporphyrin IX, mesoporphyrin IX, protoporphyrin IX, hematoporphyrin) and two related compounds (hemin, biliverdin) on the spontaneous proliferation of mouse spleen lymphocytes has been estimated in vitro by the 3H-thymidine uptake assay. It has been found that porphyrins (end...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/0006-291x(91)90522-9

    authors: Stepien H,Kunert-Radek J,Stanisz A,Zerek-Melen G,Pawlikowski M

    更新日期:1991-01-15 00:00:00

  • Ayanin diacetate-induced cell death is amplified by TRAIL in human leukemia cells.

    abstract::Here we demonstrate that the semi-synthetic flavonoid ayanin diacetate induces cell death selectively in leukemia cells without affecting the proliferation of normal lymphocytes. Incubation of human leukemia cells with ayanin diacetate induced G(2)-M phase cell cycle arrest and apoptosis which was prevented by the non...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2012.10.017

    authors: Marrero MT,Estévez S,Negrín G,Quintana J,López M,Pérez FJ,Triana J,León F,Estévez F

    更新日期:2012-11-09 00:00:00

  • Perillaldehyde attenuates cerebral ischemia-reperfusion injury-triggered overexpression of inflammatory cytokines via modulating Akt/JNK pathway in the rat brain cortex.

    abstract::Perillaldehyde (PAH), one of the major oil components in Perilla frutescens, has anti-inflammatory effects. Few studies have examined the neuroprotective effect of PAH on stroke. So the aim of our study is to investigate the effect of PAH on ischemia-reperfusion-induced injury in the rat brain cortex. Middle cerebral ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2014.10.025

    authors: Xu L,Li Y,Fu Q,Ma S

    更新日期:2014-11-07 00:00:00

  • Possible involvement of a L-delta 1-pyrroline-5-carboxylate (P5C) reductase in the synthesis of proline in Desulfovibrio desulfuricans Norway.

    abstract::A L-delta 1-pyrroline-5-carboxylate reductase activity has been detected in crude extracts of Desulfovibrio desulfuricans Norway. This P5C reductase activity is also found when a 2.5 kb D. desulfuricans DNA fragment is introduced into an Escherichia coli proC mutant. Although it restores growth of the proC mutant, the...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/0006-291x(91)91931-2

    authors: Fons M,Cami B,Chippaux M

    更新日期:1991-09-16 00:00:00

  • Aggregation of ALS-linked FUS mutant sequesters RNA binding proteins and impairs RNA granules formation.

    abstract::Protein aggregate/inclusion is one of hallmarks for neurodegenerative disorders including amyotrophic lateral sclerosis (ALS). FUS/TLS, one of causative genes for familial ALS, encodes a multifunctional DNA/RNA binding protein predominantly localized in the nucleus. C-terminal mutations in FUS/TLS cause the retention ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2014.08.115

    authors: Takanashi K,Yamaguchi A

    更新日期:2014-09-26 00:00:00

  • Loquacious-PD removes phosphate inhibition of Dicer-2 processing of hairpin RNAs into siRNAs.

    abstract::Drosophila Dicer-2 processes RNA substrates into short interfering RNAs (siRNAs). Loquacious-PD (Loqs-PD), a dsRNA-binding protein that associates with Dicer-2, is required for processing of a subset of RNA substrates including hairpin RNAs into siRNAs. Inorganic phosphate-a small molecule present in all cell types-in...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2018.03.108

    authors: Fukunaga R

    更新日期:2018-04-15 00:00:00

  • The role of wogonin in controlling SOCS3 expression in neuronal cells.

    abstract::The mechanism underlying the wogonin-mediated increase in the expression of suppressor of cytokine signaling 3 (SOCS3) is unclear. Promoter deletion assay results revealed that wogonin-induced SOCS3 expression is dependent on the AP-1 consensus sequences and two STAT responsive elements (TTACAAGAA and TTCCAGGAA) in th...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2014.07.018

    authors: Nam KW,Chae S,Song HY,Mar W,Han MD

    更新日期:2014-08-08 00:00:00

  • Ceramide-induced apoptosis is mediated by caspase activation independently from retinoblastoma protein post-translational modification.

    abstract::Recent evidence suggests that untimely retinoblastoma protein (RB) dephosphorylation and/or proteolytic degradation might provide key events down-stream cysteine protease (caspase) activation in apoptosis induction. We have dealt with this issue by studying apoptosis induced by N-hexanoylsphingosine (C6-Cer) in CHP-10...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.1998.8184

    authors: Spinedi A,Amendola A,Di Bartolomeo S,Piacentini M

    更新日期:1998-02-24 00:00:00

  • Characterization of a novel arachidonic acid-derived neutrophil chemoattractant.

    abstract::The oxidation of arachidonic acid in a superoxide-generating environment results in the formation of a potent chemoattractant that appears to be identical to a chemotactic material generated by hepatocytes when they metabolize alcohol. The product was extracted, chromatographed and characterized by physical methods in...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/s0006-291x(05)80803-4

    authors: Roll FJ,Perez HD,Serhan CN

    更新日期:1992-07-15 00:00:00

  • Purification and polymerization properties of two lethal yeast actin mutants.

    abstract::The budding yeast Saccharomyces cerevisiae contains a single actin gene and the gene product, actin, is essential for growth. Two mutants of yeast actin that do not support yeast growth were prepared from yeast by coexpressing the mutant and a 6-histidine-tagged wild-type actin followed by separation of the wild-type ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.2000.2650

    authors: Frieden C,Du J,Schriefer L,Buzan J

    更新日期:2000-05-10 00:00:00