Abstract
Kallikreins (KLKs) are secreted serine proteinases identified in a variety of cancers and in settings of inflammation.We have shown that KLKs in vitro can activate proteinase-activated receptors (PARs), a family of G-protein coupled receptors associated with inflammation. KLK14 activated both of PARs 2 and 4 and prevented thrombin from activating PAR1. On the other hand, KLK6 was a specific activator of PAR2. In an in vivo mouse inflammation model, kallikrein administration caused an oedema response comparable in magnitude and timing to that generated by trypsin. The oedema was accompanied by a decreased threshold of mechanical and thermal nociception. Our data demonstrate that by activating PARs 2 and 4 and by inactivating PAR1, widely-expressed kallikreins, like KLKs 6 and 14, may play a role in regulating the inflammatory response and pain perception.
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Oikonomopoulou, K., Hansen, K.K., Chapman, K. et al. Kallikrein-mediated activation of PARs in inflammation and nociception. Inflamm. Res. 56 (Suppl 3), S499–S502 (2007). https://doi.org/10.1007/BF03353889
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DOI: https://doi.org/10.1007/BF03353889