The role of proteases in pain

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 i...

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Bibliographic Details
Published inHandbook of experimental pharmacology Vol. 227; p. 239
Main Authors McDougall, Jason J, Muley, Milind M
Format Journal Article
LanguageEnglish
Published Germany 2015
Subjects
Animals
Humans
Pain - etiology
Pain - physiopathology
Receptors, Proteinase-Activated - antagonists & inhibitors
Receptors, Proteinase-Activated - physiology
Serine Proteases - physiology
Signal Transduction
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Summary: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.
ISSN:0171-2004
DOI:10.1007/978-3-662-46450-2_12