Navigation Links
Screening for potential beta 2-adrenergic receptor antagonists using CypHer5E and IN Cell Analyzer 1000


Introduction
CypHer5, a pH sensitive dye, has shown utility in β2-adrenergic receptor agonist screening (1). CypHer5 has been used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor expressing cells (2). For live-cell receptor internalization studies, an enhanced version of this dye, CypHer5E, has been developed (3). CypHer5E is a red-excited pH sensitive fluorogenic dye that displays minimal fluorescence at basic pH and maximal fluorescence at acidic pH. This characteristic makes it ideal for monitoring the translocation of cell surface receptors into the endosomal pathway. Such translocation is a key element of receptor trafficking and activation, particularly in G-protein coupled receptors (GPCRs) (4).

In this assay system, a CypHer5E-conjugated anti-VSV-G epitope antibody is incubated with a clonal stable HEK 293 cell line expressing N-terminally epitope tagged β2-adrenergic receptor. Upon agonist stimulation, a fluorescent signal is observed as the CypHer5E–antibody conjugate is internalized alongside the receptor into acidic endosomal vesicles.

This application note describes the validation of antagonist-format CypHer5E receptor internalization assays for high-throughput screening. A β2adrenergic receptor antagonist screen was performed using the LOPACcompound library, which consists of 640 well-characterized, pharmaceutically diverse compounds with known drug or drug-like activity. The data demonstrate that the β2-adrenergic receptor CypHer5E antagonist assay used in conjunction with IN Cell Analyzer 1000 was able to identify all specific β2-adrenergic receptor antagonists and additional structurally related compounds present in the LOPAC compound library. CypHer5E, consequently, can be used to screen for novel antagonists of known receptors and
'"/>

Source:


Page: All 1 2 3 4 5 6

Related biology technology :

1. Innovative Tissue Array Technology for High-Throughput Screening of Gene Expression
2. Screening of Beer-Spoilage Bacteria Using the LightCycler PCR Workflow System
3. LightCycler foodproof Beer Screening Kit
4. Development of a Multiplex Bead-Based Assay for Antibody Screening of a Nonhuman Primate Colony on the Bio-Plex System
5. Screening for β2-adrenergic receptor agonists using the pH-sensitive dye,CypHer5, and the IN Cell Analyzer 3000
6. A Mix-and-Read Cell-Based Assay for Hybridoma Screening Using the FMAT 8100 HTS System
7. Simultaneous Screening of 23 Drugs of Abuse in Oral Fluid Using an LC/MS/MS Method
8. Rapid Screening of Amphetamine Drugs in Urine by Positive Ion Electrospray LC/MS/MS
9. Screening of Corticosteroids in Urine by Negative Atmospheric Pressure Chemical Ionization LC/MS/MS
10. Screening and classifying hazardous waste samples
11. The development of a CXCR2 chemokine receptorbinding assay using the LEADseeker Multimodality Imaging System
Post Your Comments:
(Date:10/25/2014)... Oramed Pharmaceuticals Inc. (NASDAQCM: ORMP) ... the development of oral drug delivery systems, announced today ... present at FireRock Capital,s Micro-Cap Conference. ... Tuesday, October 28, 2014 ,Time: 9:15am EST ,Location: The ... , About The FireRock Conference  ...
(Date:10/25/2014)... 2014  RegeneRx Biopharmaceuticals, Inc. (OTCBB: RGRX) ("the Company" ... Fourth International Symposium on Thymosins in Health and Disease ... "When thymosin beta 4 (TB4) linked with rhodamine ... cavity in a rodent model of stroke, it was ... parenchyma (the functional tissue of the brain).   The leakage ...
(Date:10/25/2014)... Research and Markets has announced the addition ... Area & by End User - Global Forecast to ... In this report, the global epigenetics market is segmented ... users. The product segments of the epigenetics market included ... and reagents. The subsegments of the enzymes product segment ...
(Date:10/22/2014)... , Oct. 22, 2014 New test ... the in vitro diagnostic (IVD) test industry, especially as ... healthcare market researcher listed more than 25 testing innovations ... be the future of IVD products. Kalorama details the new ... The Worldwide Market for In Vitro Diagnostic Tests ...
Breaking Biology Technology:Oramed to Present at the FireRock Annual Micro-Cap Conference 2Oramed to Present at the FireRock Annual Micro-Cap Conference 3Researchers Report Thymosin Beta 4 Crosses Blood-Brain Barrier In Animal Stroke Model 2Global Epigenetics (VLA, WBA, NBA, RTA, Rotary-Wing Aircraft) Market - Forecast to 2019 2Global Epigenetics (VLA, WBA, NBA, RTA, Rotary-Wing Aircraft) Market - Forecast to 2019 3Report: Radical New IVD Test Approaches Key To Growth 2Report: Radical New IVD Test Approaches Key To Growth 3
... works how people can tune in to a single ... solved this week in the journal Nature by ... Psychologists have known for decades about the so-called "cocktail ... in which it was coined. It is the remarkable human ...
... are single-cell plants that comprise nature,s smallest and ... thrive is water, light, and air. When bred ... to wastewater treatment to biofuels. Current microalgae breeding ... allowed by the laws of nature. Scientists at ...
... , Expanded clinical study ...   TMC435 and BMS-986094 (formerly ... in clinical trial , ... on the development of high-value treatments for infectious diseases, ...
Cached Biology Technology:How selective hearing works in the brain 2How selective hearing works in the brain 3Medivir Announces TMC435 in an Expanded Clinical Collaboration 2Medivir Announces TMC435 in an Expanded Clinical Collaboration 3Medivir Announces TMC435 in an Expanded Clinical Collaboration 4
(Date:10/29/2014)... compete with members of their own species. However, ... into their competitive ability. Some individuals are highly ... resources, while others seem to avoid competition, instead ... are left over for them. Moreover, the degree ... to fluctuate considerably over time. A theoretical study ...
(Date:10/28/2014)... in German . ... acquire sufficient food when times are lean? By studying ... d,Ivoire researchers of the Max Planck Institute for Evolutionary ... how great apes can acquire extra energy needed to ... their sleeping nests more en route to breakfast sites ...
(Date:10/28/2014)... be building a hybrid micro-grid which will integrate ... in the region, the hybrid micro-grid will test ... diesel, storage and power-to-gas technologies, and ensure these ... built under the new Renewable Energy Integration Demonstrator- ... located offshore at Semakau Landfill and is expected ...
Breaking Biology News(10 mins):Evolution of competitiveness 2Evolution of competitiveness 3The early chimp gets the fig 2The early chimp gets the fig 3NTU to build region's first renewable energy integration demonstration micro-grid 2NTU to build region's first renewable energy integration demonstration micro-grid 3
... the growing demand for organic food products has led to ... of Science, University of Copenhagen, a European research project will ... of a food product and deciding whether or not it ... as olive oil, coffee and wine are sold at a ...
... Among overweight and obese adults, a diet rich ... and other high-fiber foods, significantly reduces markers of inflammation ... by Fred Hutchinson Cancer Research Center. Such a "low-glycemic-load" ... also increases a hormone that helps regulate the metabolism ...
... Every year, a group of anti-whaling nonprofit organizations that ... spend, by conservative estimates, some $25 million on a ... And every year, commercial whaling not only continues, but ... number of whales harvested annually has doubled since the ...
Cached Biology News:Research prevents eco-fraud 2Research prevents eco-fraud 3A diet rich in slowly digested carbs reduces markers of inflammation in overweight and obese adults 2Can we save the whales by putting a price on them? 2Can we save the whales by putting a price on them? 3
... Science Rotarods are used to assess the effect ... resistance on mice and rats using one unit ... friendly; the animals are placed on textured drums ... the individual sensing platforms below, its test results ...
... MultiScribe Reverse Transcriptase is a ... reverse transcriptase. MultiScribe Reverse Transcriptase is ... differs in its recommended usage. MuLV ... DNA polymerase that uses single-stranded RNA ...
... DNase I Amplification Grade ... DNA to oligodeoxyribonucleotides. The ... units/mg. DNAse I Amplification ... and tested for absence ...
... for the determination of digitonin and digoxin. Physical ... Na 4 and 0.06% NaCl Preparation Note: ... Biochem. Biophys. Res. Commun., 19, 755 (1965). ... of inorganic phosphorus from ATP per min at ...
Biology Products: