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Screening for Serotonin Receptor 4 Agonists Using a GPCR-Based Sensor in Yeast

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G Protein-Coupled Receptor Screening Assays

Part of the book series: Methods in Molecular Biology ((MIMB,volume 2268))

Abstract

More than 30% of all pharmaceuticals target G-protein-coupled receptors (GPCRs). Here, we present a GPCR-based screen in yeast to identify ligands for human serotonin receptor 4 (5-HTR4). Serotonin receptor 4 agonists are used for the treatment of irritable bowel syndrome with constipation. Specifically, the HTR4-based screen couples activation of 5-HTR4 on the yeast cell surface to luciferase reporter expression. The HTR4-based screen has a throughput of one compound per second allowing the screening of more than a thousand compounds per day.

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Acknowledgements

This work funded by an NIH MIRA Award (R35GM124871) to P.P-Y.

Author information

Authors and Affiliations

  1. School of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, GA, USA

    Emily A. Yasi & Pamela Peralta-Yahya

  2. School of Chemical and Biomolecular Engineering, Georgia Institute of Technology, Atlanta, GA, USA

    Pamela Peralta-Yahya

Authors
  1. Emily A. Yasi
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  2. Pamela Peralta-Yahya
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Corresponding author

Correspondence to Pamela Peralta-Yahya .

Editor information

Editors and Affiliations

  1. INESC Microsistemas e Nanotecnologias, Lisbon, Portugal

    Sofia Aires M. Martins

  2. IBB—Institute for Bioengineering and Biosciences, Lisbon, Portugal

    Duarte Miguel F. Prazeres

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Yasi, E.A., Peralta-Yahya, P. (2021). Screening for Serotonin Receptor 4 Agonists Using a GPCR-Based Sensor in Yeast. In: Martins, S.A.M., Prazeres, D.M.F. (eds) G Protein-Coupled Receptor Screening Assays. Methods in Molecular Biology, vol 2268. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-1221-7_5

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  • DOI: https://doi.org/10.1007/978-1-0716-1221-7_5

  • Published:

  • Publisher Name: Humana, New York, NY

  • Print ISBN: 978-1-0716-1220-0

  • Online ISBN: 978-1-0716-1221-7

  • eBook Packages: Springer Protocols

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