Paper identifies MOA of PAR2 antagonists

In a paper published in Nature, researchers at the Heptares Therapeutics Ltd. subsidiary of Sosei Group Corp. (Tokyo:4565) and AstraZeneca plc (LSE:AZN; NYSE:AZN) identified the binding mechanism of two protease-activated receptor 2 (PAR2) antagonists, suggesting their potential as drug candidates in multiple indications.

PAR2 is a GPCR that has been validated as a target in pain, cardiovascular disease and inflammation, but has proved difficult to modulate. When PAR2 is activated by cleavage, its extracellular domain acts as its own ligand, making it difficult to identify high affinity ligands that would lock the receptor in a stable conformation. According to BioCentury’s BCIQ database, there are no clinical compounds that target PAR2...