SPRm (Surface Plasmon Resonance Microscopy) is a novel technology that enables label-free and real-time measurements of the binding affinity and kinetics of small molecules to G protein-coupled receptors (GPCR). SPRm measurements are performed in the receptor’s physiological conditions thus providing direct and more relevant information about the binding events. Compound 13, a reported selective antagonist of GPR4, a pH-sensing receptor, has been widely used to assess the therapeutic potential of GPR4 for numerous diseases. The pH dependence and mechanism of inhibition of Compound 13 identified in the present studies highlight the limitations of this chemotype for target validation.  In this talk, we will introduce SPRm and some examples of compounds and antibody binding examples.  Dr. Rives will present the various studies with the GPR4 antagonist including pH-dependent binding studies highlighted by SPRm. Work performed and sponsored by Ferring Pharmaceuticals.

Learning Objectives:

• Describe principles of SPRm
• Review case studies of pH-dependent binding of GPR4
• Discover about label-free GPCR binding affinity and kinetics on whole cells