Surface plasmon resonance analysis of seven-transmembrane receptors

Tonia Aristotelous, Andrew L. Hopkins, Iva Navratilova (Lead / Corresponding author)

    Research output: Chapter in Book/Report/Conference proceedingChapter (peer-reviewed)peer-review

    22 Citations (Scopus)


    G-protein coupled receptors (GPCRs) are the primary target class of currently marketed drugs, accounting for around a third of all drug targets of approved medicines. However, almost all the screening efforts for novel ligand discovery rely exclusively on cellular systems overexpressing the receptors. Current receptor assay systems are based on measurement of either ligand displacement or downstream functional responses, rather than direct observation of ligand binding. Issues of allosteric modulation, probe dependence, and functional selectivity create challenges in selecting suitable assay formats. Therefore, a method that directly measures GPCR-ligand interactions, independent of binding site, probe, and signaling pathway would be a useful primary and orthogonal screening method. An alternative ligand discovery strategy would be the direct measurement of GPCR-ligand interactions by label-free technologies, such as surface plasmon resonance (SPR). In this chapter, we summarize overview of the SPR technology and development of applications for detection of ligand binding to GPCRs using wild-type and thermostabilized receptors. We discuss the utilization of SPR as a biophysical screening method for fragment-based drug discovery for GPCRs. In particular, we show how SPR screening can detect both orthosteric and allosteric ligands with the appropriate experimental design.

    Original languageEnglish
    Title of host publicationMembrane proteins—production and functional characterization
    EditorsArun K. Shukla
    PublisherAcademic Press
    Number of pages27
    ISBN (Print)9780128015216
    Publication statusPublished - 2015

    Publication series

    NameMethods in Enzymology
    PublisherAcademic Press


    • Allosteric
    • Biophysics
    • Fragment-based drug discovery
    • G-protein coupled receptors
    • Orthosteric
    • Screening
    • Surface plasmon resonance

    ASJC Scopus subject areas

    • Biochemistry
    • Molecular Biology


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