A Humanized CB1R Yeast Biosensor Enables Facile Screening of Cannabinoid Compounds

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dc.citation.articleNumber6060en_US
dc.citation.issueNumber11en_US
dc.citation.journalTitleInternational Journal of Molecular Sciencesen_US
dc.citation.volumeNumber25en_US
dc.contributor.authorMulvihill, Colleen J.en_US
dc.contributor.authorLutgens, Joshua D.en_US
dc.contributor.authorGollihar, Jimmy D.en_US
dc.contributor.authorBachanová, Petraen_US
dc.contributor.authorTramont, Caitlinen_US
dc.contributor.authorMarcotte, Edward M.en_US
dc.contributor.authorEllington, Andrew D.en_US
dc.contributor.authorGardner, Elizabeth C.en_US
dc.date.accessioned2024-08-02T13:32:09Zen_US
dc.date.available2024-08-02T13:32:09Zen_US
dc.date.issued2024en_US
dc.description.abstractYeast expression of human G-protein-coupled receptors (GPCRs) can be used as a biosensor platform for the detection of pharmaceuticals. Cannabinoid receptor type 1 (CB1R) is of particular interest, given the cornucopia of natural and synthetic cannabinoids being explored as therapeutics. We show for the first time that engineering the N-terminus of CB1R allows for efficient signal transduction in yeast, and that engineering the sterol composition of the yeast membrane modulates its performance. Using an engineered cannabinoid biosensor, we demonstrate that large libraries of synthetic cannabinoids and terpenes can be quickly screened to elucidate known and novel structure–activity relationships. The biosensor strains offer a ready platform for evaluating the activity of new synthetic cannabinoids, monitoring drugs of abuse, and developing therapeutic molecules.en_US
dc.identifier.citationMulvihill, C. J., Lutgens, J. D., Gollihar, J. D., Bachanová, P., Tramont, C., Marcotte, E. M., Ellington, A. D., & Gardner, E. C. (2024). A Humanized CB1R Yeast Biosensor Enables Facile Screening of Cannabinoid Compounds. International Journal of Molecular Sciences, 25(11), Article 11. https://doi.org/10.3390/ijms25116060en_US
dc.identifier.digitalijms-25-06060en_US
dc.identifier.doihttps://doi.org/10.3390/ijms25116060en_US
dc.identifier.urihttps://hdl.handle.net/1911/117571en_US
dc.language.isoengen_US
dc.publisherMDPIen_US
dc.rightsExcept where otherwise noted, this work is licensed under a Creative Commons Attribution (CC BY) license.  Permission to reuse, publish, or reproduce the work beyond the terms of the license or beyond the bounds of fair use or other exemptions to copyright law must be obtained from the copyright holder.en_US
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/en_US
dc.titleA Humanized CB1R Yeast Biosensor Enables Facile Screening of Cannabinoid Compoundsen_US
dc.typeJournal articleen_US
dc.type.dcmiTexten_US
dc.type.publicationpublisher versionen_US
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