Fragment screening by SPR and advanced application to GPCRs.

摘要: Surface plasmon resonance (SPR) is one of the primary biophysical methods for screening low molecular weight 'fragment' libraries, due to its protein consumption and 'label-free' methodology. SPR biosensor interaction analysis employed both screen confirm binding compounds in fragment experiments, as it provides accurate information on affinity kinetics interactions. The most advanced application use against membrane drug targets, such G-protein coupled receptors (GPCRs). Biophysical GPCR assays using have been validated with pharmacological measurements approximate cell-based methods, yet provide advantage their ability measure weak affinities fragments. A number screens GPCRs now disclosed literature. proving versatile thermostabilised solubilised wild type receptors. In this chapter, we discuss state-of-the-art by technical considerations performing experiments.