Evidence map›Paper›PMID 22767611›Full record

ArticleMolecular pharmacology2012

Discovery of regulators of receptor internalization with high-throughput flow cytometry.

Yang Wu, Phillip H Tapia, Gregory W Fisher, Peter C Simons, J Jacob Strouse, Terry Foutz, Alan S Waggoner, Jonathan Jarvik, Larry A Sklar

Abstract readValidation Study
In one paragraph

Article in Molecular pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

11 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
  4. Fluorogenic Labeling Strategies for Biological Imaging.International journal of molecular sciences · 2017
    Review
  5. Article
  6. Dark dyes-bright complexes: fluorogenic protein labeling.Current opinion in chemical biology · 2015
    Review
  7. Article
  8. Article
  9. Article
  10. High-throughput flow cytometry compatible biosensor based on fluorogen activating protein technology.Cytometry. Part A : the journal of the International Society for Analytical Cytology · 2013
    Article
  11. Article
4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

9 authors.

Yang WuDepartment of Pathology, School of Medicine, University of New Mexico, MSC08 4640, 700 Camino de Salud NE, IDTC Rm 2340, Albuquerque, NM 87131, USA. yawu@salud.unm.edu
Phillip H Tapia
Gregory W Fisher
Peter C Simons
J Jacob Strouse
Terry Foutz
Alan S Waggoner
Jonathan Jarvik
Larry A Sklar

Funding

FLUORESCENT PROBES &IMAGING FOR NETWORKS &PATHWAY(RMI)U54RR022241 · NCRR · MELLON PITTS CORPORATION (MPC CORP) · PI WAGGONER, ALAN S. · 2005 to 2011
$19.9M
Yeast Biology ConsortiumU54MH084690 · NIMH · UNIVERSITY OF NEW MEXICO HEALTH SCIS CTR · PI SKLAR, LARRY A. · 2008 to 2013
$14.4M
Fluorescent Biosensors for Networks and PathwaysU54GM103529 · NIGMS · CARNEGIE-MELLON UNIVERSITY · PI WAGGONER, ALAN S. · 2012 to 2013
$6.3M
HTS FOR NON-CANONICAL LIGANDS FOR BETA 2 ADRENERGIC RECEPTOR INTERNALIZATIONR03DA031668 · NIDA · CARNEGIE-MELLON UNIVERSITY · PI JARVIK, JONATHAN W · 2011 to 2012
$74k
NCRR NIH HHS 5U54-RR022241NCRR NIH HHS U54 RR022241NIDA NIH HHS R03 DA031668NIGMS NIH HHS U54 GM103529NIMH NIH HHS 1R03-MH093192NIMH NIH HHS 1U54-MH084690-02NIMH NIH HHS 5U54-MH084690-03NIMH NIH HHS U54 MH084690
6 · The paper itself

Abstract

We developed a platform combining fluorogen-activating protein (FAP) technology with high-throughput flow cytometry to detect real-time protein trafficking to and from the plasma membrane in living cells. The hybrid platform facilitates drug discovery for trafficking receptors such as G protein-coupled receptors and was validated with the β₂-adrenergic receptor (β₂AR) system. When a chemical library containing ∼1200 off-patent drugs was screened against cells expressing FAP-tagged β₂ARs, all 33 known β₂AR-active ligands in the library were successfully identified, together with a number of compounds that might regulate receptor internalization in a nontraditional manner. Results indicated that the platform identified ligands of target proteins regardless of the associated signaling pathway; therefore, this approach presents opportunities to search for biased receptor modulators and is suitable for screening of multiplexed targets for improved efficiency. The results revealed that ligands may be biased with respect to the rate or duration of receptor internalization and that receptor internalization may be independent of activation of the mitogen-activated protein kinase pathway.

Indexed as

Adrenergic beta-2 Receptor AgonistsAdrenergic beta-2 Receptor AntagonistsBinding, CompetitiveFlow CytometryGreen Fluorescent ProteinsHigh-Throughput Screening AssaysHumansLigandsProtein TransportReceptors, Adrenergic, beta-2Receptors, G-Protein-CoupledRecombinant Fusion ProteinsSmall Molecule LibrariesTime FactorsTransfectionU937 CellsAdrenergic beta-2 Receptor AgonistsAdrenergic beta-2 Receptor AntagonistsGreen Fluorescent ProteinsLigandsReceptors, Adrenergic, beta-2Receptors, G-Protein-CoupledRecombinant Fusion ProteinsSmall Molecule Libraries

Identifiers

PMID22767611
PMCPMC3463215

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.