Screening for GPCR Ligands Using Surface Plasmon Resonance.

ABSTRACT: G-protein coupled receptors (GPCRs) are a class of drug targets of primary importance. However, receptor assays 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 assays 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. We have developed a GPCR biosensor assay protocol that offers the opportunity for high-throughput label-free screening that directly measures GPCR-ligand interactions. The biosensor-based direct screening method identifies the

SUBMITTER: Navratilova I 

PROVIDER: S-EPMC3137231 | biostudies-literature | 2011 Jul

REPOSITORIES: biostudies-literature