Second annual GPCRs: from orphan to blockbuster.

The superfamily of G-protein-coupled receptors (GPCRs) was discussed at a recent Cambridge Healthtech Institute meeting. Scientists working in both academia and industry participated in 2 days of talks that addressed important issues related to the use of GPCRs as targets. The meeting delved into questions and strategies surrounding receptor structure, lack of knowledge about endogenous ligands, novel methodology for identifying compounds from high-throughput screening, the development process from hits to leads, and what constitutes adequate proof-of-principle studies. This report highlights several presentations related to the ongoing search for more effective GPCR-targeted drug discovery efforts.