Resumen de To bind or not to bind: unravelling GPCR polypharmacology

Patrick M. Sexton, Arthur Christopoulos

• Interaction of a single drug with multiple targets through “polypharmacology” is increasingly recognized as necessary for treatment of complex diseases, such as schizophrenia. G protein-coupled receptors (GPCRs) are major medicinal targets, and understanding the structural basis of both GPCR drug selectivity and promiscuity could provide novel avenues for drug development.