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Visualising ligand-binding to a GPCR in vivo using nanoBRET

Carvalheira Alcobia, Diana; Ziegler, Alexandra I.; Kondrashov, Alexander; Comeo, Eleonora; Mistry, Sarah; Kellam, Barrie; Chang, Aeson; Woolard, Jeannette; Hill, Stephen J.; Sloan, Erica K.

Authors

Diana Carvalheira Alcobia

Alexandra I. Ziegler

Eleonora Comeo

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BARRIE KELLAM BARRIE.KELLAM@NOTTINGHAM.AC.UK
Professor of Medicinal Chemistry

Aeson Chang

JEANETTE WOOLARD Jeanette.Woolard@nottingham.ac.uk
Professor of Cardiovascular Physiology and Pharmacology

STEPHEN HILL STEVE.HILL@NOTTINGHAM.AC.UK
Professor of Molecular Pharmacology

Erica K. Sloan



Abstract

© 2018 The Author(s) The therapeutic action of a drug depends on its ability to engage with its molecular target in vivo. However, current drug discovery strategies quantify drug levels within organs rather than determining the binding of drugs directly to their specific molecular targets in vivo. This is a particular problem for assessing the therapeutic potential of drugs that target malignant tumors where access and binding may be impaired by disrupted vasculature and local hypoxia. Here we have used triple-negative human breast cancer cells expressing β2-adrenoceptors tagged with the bioluminescence protein NanoLuc to provide a bioluminescence resonance energy transfer approach to directly quantify ligand binding to a G protein-coupled receptor in vivo using a mouse model of breast cancer.

Citation

Carvalheira Alcobia, D., Ziegler, A. I., Kondrashov, A., Comeo, E., Mistry, S., Kellam, B., …Sloan, E. K. (2018). Visualising ligand-binding to a GPCR in vivo using nanoBRET. iScience, 6(8), 280-288. https://doi.org/10.1016/j.isci.2018.08.006

Journal Article Type Article
Acceptance Date Aug 6, 2018
Online Publication Date Aug 11, 2018
Publication Date Aug 31, 2018
Deposit Date Aug 9, 2018
Publicly Available Date Mar 29, 2024
Journal iScience
Electronic ISSN 2589-0042
Publisher Elsevier (Cell Press)
Peer Reviewed Peer Reviewed
Volume 6
Issue 8
Pages 280-288
DOI https://doi.org/10.1016/j.isci.2018.08.006
Public URL https://nottingham-repository.worktribe.com/output/986075
Publisher URL https://www.sciencedirect.com/science/article/pii/S2589004218301184
Additional Information This article is maintained by: Elsevier; Article Title: Visualizing Ligand Binding to a GPCR InVivo Using NanoBRET; Journal Title: iScience; CrossRef DOI link to publisher maintained version: https://doi.org/10.1016/j.isci.2018.08.006; Content Type: article; Copyright: © 2018 The Author(s).

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