Emerging role of surface plasmon resonance in fragment-based drug discovery

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    46 Citations (Scopus)

    Abstract

    Surface plasmon resonance (SPR) offers a method of biophysical fragment screening that is fast, efficient, cost effective and accurate. SPR is increasingly being adopted as a secondary assay to validate fragment hits. Recently, technical advances have resulted in the emergence of SPR as a primary screening methodology for fragment-based drug discovery. Moreover, SPR biosensor assays can be developed for a wide range of proteins, including membrane proteins, such as G-protein-coupled receptors. In this review, we discuss the advantages and limitations of SPR fragment screening including experimental consideration of reducing false positive and false negative rates to a minimum. We discuss how ligand efficiency can be used both as a method to eliminate false positives and to understand which fragments in a library may be a source of false negatives.

    Original languageEnglish
    Pages (from-to)1809-1820
    Number of pages12
    JournalFuture Medicinal Chemistry
    Volume3
    Issue number14
    DOIs
    Publication statusPublished - Oct 2011

    Keywords

    • PROTEIN-COUPLED RECEPTORS
    • LEAD DISCOVERY
    • BIOSENSOR TECHNOLOGY
    • TARGET INTERACTIONS
    • BIACORE TECHNOLOGY
    • BINDING
    • AFFINITY
    • DESIGN
    • NMR
    • SPR

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