The role of proteases in pain.

Jason J McDougall, Milind M Muley

Handbook of experimental pharmacology 2015

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Proteinase-activated receptors (PARs) are a family of G protein-coupled receptor that are activated by extracellular cleavage of the receptor in the N-terminal domain. This slicing of the receptor exposes a tethered ligand which binds to a specific docking point on the receptor surface to initiate intracellular signalling. PARs are expressed by numerous tissues in the body, and they are involved in various physiological and pathological processes such as food digestion, tissue remodelling and blood coagulation. This chapter will summarise how serine proteinases activate PARs leading to the development of pain in several chronic pain conditions. The potential of PARs as a drug target for pain relief is also discussed.