Evidence map›Paper›PMID 25116377›Full record

ArticleJournal of the American Chemical Society2014

Programmable nanoscaffolds that control ligand display to a G-protein-coupled receptor in membranes to allow dissection of multivalent effects.

Andrew V Dix, Steven M Moss, Khai Phan, Travis Hoppe, Silvia Paoletta, Eszter Kozma, Zhan-Guo Gao, Stewart R Durell, Kenneth A Jacobson, Daniel H Appella

Abstract read
In one paragraph

Article in Journal of the American Chemical Society, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing 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

9 citing papers in PubMed.

  1. Article
  2. Review
  3. Review
  4. Article
  5. Article
  6. Article
  7. New paradigms in GPCR drug discovery.Biochemical pharmacology · 2015
    Review
  8. Article
  9. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors.

Andrew V DixLaboratory of Bioorganic Chemistry, NIDDK, ‡Laboratory of Biochemistry and Genetics, NIDDK, and §Laboratory of Cell Biology, CCR, NCI, National Institutes of Health , Bethesda, Maryland 20892, United States.
Steven M Moss
Khai Phan
Travis Hoppe
Silvia Paoletta
Eszter Kozma
Zhan-Guo Gao
Stewart R Durell
Kenneth A Jacobson
Daniel H Appella

Funding

Chemically Modified Peptide Nucleic AcidsZIADK031143 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI APPELLA, DANIEL H · 2009 to 2025
$13.9M
Functionalized Congeners Of Bioactive CompoundsZIADK031115 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 2009 to 2025
$5.3M
Intramural NIH HHS
6 · The paper itself

Abstract

A programmable ligand display system can be used to dissect the multivalent effects of ligand binding to a membrane receptor. An antagonist of the A2A adenosine receptor, a G-protein-coupled receptor that is a drug target for neurodegenerative conditions, was displayed in 35 different multivalent configurations, and binding to A2A was determined. A theoretical model based on statistical mechanics was developed to interpret the binding data, suggesting the importance of receptor dimers. Using this model, extended multivalent arrangements of ligands were constructed with progressive improvements in binding to A2A. The results highlight the ability to use a highly controllable multivalent approach to determine optimal ligand valency and spacing that can be subsequently optimized for binding to a membrane receptor. Models explaining the multivalent binding data are also presented.

Indexed as

Adenosine A2 Receptor AntagonistsBinding SitesDNAHumansLigandsModels, MolecularNanostructuresPeptide Nucleic AcidsProtein BindingReceptor, Adenosine A2AAdenosine A2 Receptor AntagonistsDNALigandsPeptide Nucleic AcidsReceptor, Adenosine A2A

Identifiers

PMID25116377
PMCPMC4156868

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.