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Review ARTICLE Provisionally accepted The full-text will be published soon. Notify me

Front. Endocrinol. | doi: 10.3389/fendo.2019.00717

Protease-activated receptors in the intestine: focus on inflammation and cancer

  • 1INSERM U1220 Institut de Recherche en Santé Digestive, France
  • 2Centre Hospitalier Universitaire de Toulouse, France

Protease-activated receptors (PARs) belong to the G protein-coupled receptor (GPCR) family. Compared to others GPCRs, the specificity of the four PARs is the lack of physiologically soluble ligands. Indeed, PARs are physiologically activated after proteolytic cleavage of their N-terminal domain by proteases. The resulting N-terminal end becomes a tethered activation ligand that interact with the extracellular loop 2 domain and thus induce PAR signal.
PARs expression is ubiquitous and these receptors have been largely described in chronic inflammatory diseases and cancer. In this review, after describing their discovery, structure, mechanisms of activation, we then focus on the roles of PARs in the intestine and the two main diseases affecting the organ, namely inflammatory bowel disease and cancer.

Keywords: Protease-activated receptors (PARs), intestine, Inflammation, Cancer, signaling

Received: 09 Jul 2019; Accepted: 04 Oct 2019.

Copyright: © 2019 SEBERT, Solà Tapias, MAS, BARREAU and FERRAND. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

* Correspondence: Dr. Audrey FERRAND, INSERM U1220 Institut de Recherche en Santé Digestive, Toulouse, France, audrey.ferrand@inserm.fr