ArticleChemical science2018
High-throughput identification of G protein-coupled receptor modulators through affinity mass spectrometry screening.
Article in Chemical science, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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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.
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.
Who cites it
20 citing papers in PubMed, 47 citations in OpenAlex.
- Breaking the boundaries of affinity selection-mass spectrometry: From ligand screening to target-ligand interaction insights.Journal of pharmaceutical analysis · 2026Review
- Expanding the Reach of Membrane Protein-Ligand Interaction Studies Through the Integration of Mass Spectrometry and Membrane Mimetics.Proteomics · 2025Review
- Article
- Genome-wide pan-GPCR cell libraries accelerate drug discovery.Acta pharmaceutica Sinica. B · 2024Review
- 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 · 2023Article
- Rapid One-Step Capturing of Native, Cell-Free Synthesized and Membrane-Embedded GLP-1R.International journal of molecular sciences · 2023Article
- High-throughput screening strategies for space-based radiation countermeasure discovery.Life sciences in space research · 2022Review
- Article
- Review
- Inhibitors Targeting Multiple Janus Kinases FromFrontiers in chemistry · 2022Article
- Drug discovery from natural products using affinity selection-mass spectrometry.Drug discovery today. Technologies · 2021Review
- Discovery of Novel Allosteric Modulators Targeting an Extra-Helical Binding Site of GLP-1R Using Structure- and Ligand-Based Virtual Screening.Biomolecules · 2021Article
- Discovery and characterization of naturally occurring potent inhibitors of catechol-RSC advances · 2021Article
- G protein-coupled receptors: structure- and function-based drug discovery.Signal transduction and targeted therapy · 2021Review
- Exploring new targets and chemical space with affinity selection-mass spectrometry.Nature reviews. Chemistry · 2021Review
- Advances in G protein-coupled receptor high-throughput screening.Current opinion in biotechnology · 2020Review
- A Novel G Protein-Biased and Subtype-Selective Agonist for a G Protein-Coupled Receptor Discovered from Screening Herbal Extracts.ACS central science · 2020Article
- Residues and residue pairs of evolutionary importance differentially direct signaling bias of D2 dopamine receptors.The Journal of biological chemistry · 2019Article
- Accelerating the Throughput of Affinity Mass Spectrometry-Based Ligand Screening toward a G Protein-Coupled Receptor.Analytical chemistry · 2019Article
- Emerging Paradigm of Intracellular Targeting of G Protein-Coupled Receptors.Trends in biochemical sciences · 2018Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
20 authors at 5 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
G protein-coupled receptors (GPCRs) represent the largest class of cell surface proteins and thus constitute an important family of therapeutic targets. Therefore, significant effort has been put towards the identification of novel ligands that can modulate the activity of a GPCR target with high efficacy and selectivity. However, due to limitations inherent to the most common techniques for GPCR ligand discovery, there is a pressing need for more efficient and effective ligand screening methods especially for the identification of potential allosteric modulators. Here we present a high-throughput, label-free and unbiased screening approach for the identification of small molecule ligands towards GPCR targets based on affinity mass spectrometry. This new approach features the usage of target-expressing cell membranes rather than purified proteins for ligand screening and allows the detection of both orthosteric and allosteric ligands targeting specific GPCRs. Screening a small compound library with this approach led to the rapid discovery of an antagonist for the 5-HT receptor and four positive allosteric modulators for GLP-1 receptor that were not previously reported.
Identifiers
What OpenQuestion holds
Registered trials
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.