Visualizing Ligand Binding to a GPCR In Vivo Using NanoBRET

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

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)


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.
Original languageEnglish
Pages (from-to)280-288
Number of pages9
Publication statusPublished - 31 Aug 2018


  • Biological Sciences Tools
  • Cancer
  • Molecular Interaction
  • Optical Imaging

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