ArticleScientific reports2019
High-throughput identification of peptide agonists against GPCRs by co-culture of mammalian reporter cells and peptide-secreting yeast cells using droplet microfluidics.
Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 27 citations in OpenAlex.
- Integrating fab phage and yeast display through seamless transfer of paired heavy- and light-chain libraries for efficient antibody discovery.Antibody therapeutics · 2026Article
- The adaptive immune receptors in a big data world.ImmunoHorizons · 2026Review
- Three-tier framework for high-throughput biofabrication: Integrating 3D bioprinting, assistive platforms, and translational opportunities.Bioactive materials · 2026Review
- Genome-wide pan-GPCR cell libraries accelerate drug discovery.Acta pharmaceutica Sinica. B · 2024Review
- Technologies for the discovery of G protein-coupled receptor-targeting biologics.Current opinion in biotechnology · 2024Review
- Droplet-based microfluidic platform for detecting agonistic peptides that are self-secreted by yeast expressing a G-protein-coupled receptor.Microbial cell factories · 2024Article
- Deep mutational scanning of proteins in mammalian cells.Cell reports methods · 2023Review
- Drosophila CASK regulates brain size and neuronal morphogenesis, providing a genetic model of postnatal microcephaly suitable for drug discovery.Neural development · 2023Article
- Export of Diverse and Bioactive Small Proteins through a Type I Secretion System.Applied and environmental microbiology · 2023Article
- Fungi-on-a-Chip: microfluidic platforms for single-cell studies on fungi.FEMS microbiology reviews · 2022Review
- Enrichment of gut microbiome strains for cultivation-free genome sequencing using droplet microfluidics.Cell reports methods · 2022Article
- Agonist antibody discovery: Experimental, computational, and rational engineering approaches.Drug discovery today · 2022Review
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- Article
- Minireview: Novel Micropeptide Discovery by Proteomics and Deep Sequencing Methods.Frontiers in genetics · 2021Review
- Design, Screening, and Testing of Non-Rational Peptide Libraries with Antimicrobial Activity: In Silico and Experimental Approaches.Antibiotics (Basel, Switzerland) · 2020Review
- Advances in G protein-coupled receptor high-throughput screening.Current opinion in biotechnology · 2020Review
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Since G-protein coupled receptors (GPCRs) are linked to various diseases, screening of functional ligands against GPCRs is vital for drug discovery. In the present study, we developed a high-throughput functional cell-based assay by combining human culture cells producing a GPCR, yeast cells secreting randomized peptide ligands, and a droplet microfluidic device. We constructed a reporter human cell line that emits fluorescence in response to the activation of human glucagon-like peptide-1 receptor (hGLP1R). We then constructed a yeast library secreting an agonist of hGLP1R or randomized peptide ligands. We demonstrated that high-throughput identification of functional ligands against hGLP1R could be performed by co-culturing the reporter cells and the yeast cells in droplets. We identified functional ligands, one of which had higher activity than that of an original sequence. The result suggests that our system could facilitate the discovery of functional peptide ligands of GPCRs.
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Registered trials
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