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Effector membrane translocation biosensors reveal G protein and βarrestin coupling profiles of 100 therapeutically relevant GPCRs
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Abstract
The recognition that individual GPCRs can activate multiple signaling pathways has raised the possibility of developing drugs selectively targeting therapeutically relevant ones. This requires tools to determine which G proteins and βarrestins are activated by a given receptor. Here, we present a set of BRET sensors monitoring the activation of the 12 G protein subtypes based on the translocation of their effectors to the plasma membrane (EMTA). Unlike most of the existing detection systems, EMTA does not require modification of receptors or G proteins (except for G s ). EMTA was found to be suitable for the detection of constitutive activity, inverse agonism, biased signaling and polypharmacology. Profiling of 100 therapeutically relevant human GPCRs resulted in 1500 pathway-specific concentration-response curves and revealed a great diversity of coupling profiles ranging from exquisite selectivity to broad promiscuity. Overall, this work describes unique resources for studying the complexities underlying GPCR signaling and pharmacology.
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Cites
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Self-citation
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Metadata
- Authors
- Avet, C., Mancini, A., Breton, B., Le Gouill, C., Hauser, A. S., Normand, C., Kobayashi, H., Gross, F., Hogue, M., Lukasheva, V., St-Onge, S., Carrier, M., Héroux, M., Morissette, S., Fauman, E. B., Fortin, J.-P., Schann, S., Leroy, X., Gloriam, D. E., & Bouvier, M.
- Venue
- eLife
- Publisher
- eLife Sciences Publications, Ltd
- Published
- 2022-03-18
- Volume
- 11
- ISSN
- 2050-084X (ISSN-L)
- OpenAlex
- W4220763721
- Cited by
- 267
- References
- 57
- FWCI
- 14.64
- Type
- journal article
- Language
- en
- Open access
- gold
- Licence
- creativecommons.org/licenses/by/4.0/ (vor)
- creativecommons.org/licenses/by/4.0/ (am)
- creativecommons.org/licenses/by/4.0/ (tdm)
- Funders
- Canada Research Chairs
- Canadian Institutes of Health Research (FDN-148431)
- Lundbeckfonden (R218-2016-1266, R313-2019-526, R278-2018-180)
- Novo Nordisk Fonden (NNF18OC0031226)
- Bristol-Myers Squibb
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- The paper
- Avet, C., Mancini, A., Breton, B., Le Gouill, C., Hauser, A. S., Normand, C., Kobayashi, H., Gross, F., Hogue, M., Lukasheva, V., St-Onge, S., Carrier, M., Héroux, M., Morissette, S., Fauman, E. B., Fortin, J.-P., Schann, S., Leroy, X., Gloriam, D. E., & Bouvier, M. (2022). Effector membrane translocation biosensors reveal G protein and βarrestin coupling profiles of 100 therapeutically relevant GPCRs. eLife. https://doi.org/10.7554/elife.74101
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
