Evidence map›Paper›PMID 31094506›Full record

ArticleAnalytical chemistry2019

Accelerating the Throughput of Affinity Mass Spectrometry-Based Ligand Screening toward a G Protein-Coupled Receptor.

Yan Lu, Shanshan Qin, Bingjie Zhang, Antao Dai, Xiaoqing Cai, Mengna Ma, Zhan-Guo Gao, Dehua Yang, Raymond C Stevens, Kenneth A Jacobson and 2 more

Erratum issuedOpen access · greenAbstract read
In one paragraph

Article in Analytical chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing papers in PubMed
1.5field-weighted citation impact, top 17% of its field
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

17 citing papers in PubMed, 39 citations in OpenAlex.

  1. Article
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  8. Affinity selection of double-click triazole libraries for rapid discovery of allosteric modulators for GLP-1 receptor.Proceedings of the National Academy of Sciences of the United States of America · 2023
    Article
  9. Review
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  11. Adenosine ABritish journal of pharmacology · 2022
    Review
  12. Article
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4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

12 authors at 4 institutions in 2 countries.

Yan LuiHuman Institute , ShanghaiTech University , 201210 Shanghai , China.
Shanshan QiniHuman Institute , ShanghaiTech University , 201210 Shanghai , China.
Bingjie ZhangiHuman Institute , ShanghaiTech University , 201210 Shanghai , China.
Antao DaiThe National Center for Drug Screening and the CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica , Chinese Academy of Sciences , 201203 Shanghai , China.
Xiaoqing CaiThe National Center for Drug Screening and the CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica , Chinese Academy of Sciences , 201203 Shanghai , China.
Mengna MaiHuman Institute , ShanghaiTech University , 201210 Shanghai , China.
Zhan-Guo GaoNational Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) , National Institutes of Health , Bethesda , Maryland 20892 United States.
Dehua YangThe National Center for Drug Screening and the CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica , Chinese Academy of Sciences , 201203 Shanghai , China.
Raymond C StevensiHuman Institute , ShanghaiTech University , 201210 Shanghai , China.
Kenneth A JacobsonNational Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) , National Institutes of Health , Bethesda , Maryland 20892 United States.ORCID 0000-0001-8104-1493
Ming-Wei WangUniversity of Chinese Academy of Sciences , 100049 Beijing , China.
Wenqing ShuiiHuman Institute , ShanghaiTech University , 201210 Shanghai , China.ORCID 0000-0002-5245-2477
ShanghaiTech University · CNShanghai Institute of Materia Medica · CNNational Institutes of Health · USFudan University · CN

Funding

Development Of Drugs Acting At Adenosine ReceptorsZIADK031117 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 2009 to 2025
$10.4M
Computer Modeling of G Protein-Coupled ReceptorsZIADK031126 · NIDDK · NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES · PI JACOBSON, KENNETH ALAN · 2009 to 2025
$6.6M
Intramural NIH HHS ZIA DK031117
6 · The paper itself

Abstract

Affinity mass spectrometry (MS) enables rapid screening of compound mixtures for ligands bound to a specific protein target, yet its current throughput is limited to individually assay pools of 400-2000 compounds. Typical affinity MS screens implemented in pharmaceutical industry laboratories identify putative ligands based on qualitative analysis of compound binding to the target whereas no quantitative information is acquired to discriminate high- and low-affinity ligands in the screening phase. Furthermore, these screens require purification of a stabilized form of the protein target, which poses a great challenge for membrane receptor targets. Here, we describe a new, potentially general affinity MS strategy that allows screening of 20,000 compounds in one pool for highly efficient ligand discovery toward a G protein-coupled receptor (GPCR) target. Quantitative measurement of compound binding to the receptor enables high-affinity ligand selection using both the purified receptor and receptor-embedded cell membranes. This high-throughput, label-free and quantitative affinity MS screen resulted in discovery of three new antagonists of the A

Indexed as

Adenosine A2 Receptor AntagonistsCell MembraneHigh-Throughput Screening AssaysHumansLigandsMass SpectrometryProtein BindingReceptors, G-Protein-CoupledAdenosine A2 Receptor AntagonistsLigandsReceptors, G-Protein-Coupled

Identifiers

PMID31094506
PMCPMC6669887
OpenAlexW2946364931

What OpenQuestion holds

Textmetadata
LicenceTDM
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.