Structural insight into allosteric modulation of protease-activated receptor 2

Crystal structures of protease-activated receptor 2 (PAR2) in complex with two different antagonist ligands and with a blocking antibody reveal binding sites that are distinct from those found on PAR1, offering new leads for structure-based drug design. Protease-activated receptors (PARs) are a family of G-protein-coupled receptors (GPCRs) with roles in diverse diseases, such as neuroinflammation and cancer, and are considered important target...