ArticleCommunications biology2020
Function-based high-throughput screening for antibody antagonists and agonists against G protein-coupled receptors.
Article in Communications biology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
What it found
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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.
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Who cites it
25 citing papers in PubMed, 38 citations in OpenAlex.
- Article
- De novo design of miniproteins targeting GPCRs.Nature · 2026Article
- The evolution of display technologies for antibody drug discovery.Trends in biotechnology · 2026Review
- International Union of Basic and Clinical Pharmacology. CXXI. Apelin receptor pharmacology in the human cardiovascular system and emerging clinical applications.Pharmacological reviews · 2026Review
- Nanobodies unlock new mechanisms to target G protein-coupled receptors.Molecular pharmacology · 2026Review
- An efficient functional screening method for anti ATP hydrolase antibody based on fluorescent probes.Frontiers in immunology · 2026Article
- Engineering mammalian protein secretion: Toward the convergence of high-throughput biology and computational methods.Cell systems · 2025Review
- Article
- Phage Display as a Medium for Target Therapy Based Drug Discovery, Review and Update.Molecular biotechnology · 2025Review
- Bacteriophage-based strategies for biocontrol and treatment of infectious diseases.Computational and structural biotechnology journal · 2025Review
- Structure elucidation of a human melanocortin-4 receptor specific orthosteric nanobody agonist.Nature communications · 2024Article
- Technologies for the discovery of G protein-coupled receptor-targeting biologics.Current opinion in biotechnology · 2024Review
- High-fidelity large-diversity monoclonal mammalian cell libraries by cell cycle arrested recombinase-mediated cassette exchange.Nucleic acids research · 2023Article
- Discovery of Potent and Selective CB2 Agonists Utilizing a Function-Based Computational Screening Protocol.ACS chemical neuroscience · 2023Article
- Deep Antimicrobial Activity and Stability Analysis Inform Lysin Sequence-Function Mapping.ACS synthetic biology · 2023Article
- Improving antibody drug development using bionanotechnology.Current opinion in biotechnology · 2022Review
- Agonist antibody discovery: Experimental, computational, and rational engineering approaches.Drug discovery today · 2022Review
- Intracellular VHHs to monitor and modulate GPCR signaling.Frontiers in endocrinology · 2022Review
- Accelerating GPCR Drug Discovery With Conformation-Stabilizing VHHs.Frontiers in molecular biosciences · 2022Review
- Activation of a G protein-coupled receptor through indirect antibody-mediated tethering of ligands.RSC chemical biology · 2021Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Hybridoma and phage display are two powerful technologies for isolating target-specific monoclonal antibodies based on the binding. However, for complex membrane proteins, such as G protein-coupled receptors (GPCRs), binding-based screening rarely results in functional antibodies. Here we describe a function-based high-throughput screening method for quickly identifying antibody antagonists and agonists against GPCRs by combining glycosylphosphatidylinositol-anchored antibody cell display with β-arrestin recruitment-based cell sorting and screening. This method links antibody genotype with phenotype and is applicable to all GPCR targets. We validated this method by identifying a panel of antibody antagonists and an antibody agonist to the human apelin receptor from an immune antibody repertoire. In contrast, we obtained only neutral binders and antibody antagonists from the same repertoire by phage display, suggesting that the new approach described here is more efficient than traditional methods in isolating functional antibodies. This new method may create a new paradigm in antibody drug discovery.
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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.