title: Emerging role of surface plasmon resonance in fragment-based drug discovery.
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.
authors: Division of Biological Chemistry & Drug Discovery, College of Life Sciences, University of Dundee, Dow Street, Dundee, DD1 5EH, UK. i.navratilova@dundee.ac.uk
authors: Iva
authors: I
authors: Navratilova
authors: Andrew L
authors: AL
authors: Hopkins
mesh_terms: D015374:Biosensing Techniques; D055808:Drug Discovery; D008565:Membrane Proteins / Q000187:drug effects; D020349:Surface Plasmon Resonance / Q000706:statistics & numerical data*
chemical_list: D008565:Membrane Proteins