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Protease-Activated Receptors in the Intestine: Focus on Inflammation and Cancer

Protease-activated receptors (PARs) belong to the G protein-coupled receptor (GPCR) family. Compared to other GPCRs, the specificity of the four PARs is the lack of physiologically soluble ligands able to induce their activation. Indeed, PARs are physiologically activated after proteolytic cleavage...

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Autores principales: Sébert, Morgane, Sola-Tapias, Nuria, Mas, Emmanuel, Barreau, Frédérick, Ferrand, Audrey
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6821688/
https://www.ncbi.nlm.nih.gov/pubmed/31708870
http://dx.doi.org/10.3389/fendo.2019.00717
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author Sébert, Morgane
Sola-Tapias, Nuria
Mas, Emmanuel
Barreau, Frédérick
Ferrand, Audrey
author_facet Sébert, Morgane
Sola-Tapias, Nuria
Mas, Emmanuel
Barreau, Frédérick
Ferrand, Audrey
author_sort Sébert, Morgane
collection PubMed
description Protease-activated receptors (PARs) belong to the G protein-coupled receptor (GPCR) family. Compared to other GPCRs, the specificity of the four PARs is the lack of physiologically soluble ligands able to induce their activation. 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 diseases and cancer.
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spelling pubmed-68216882019-11-08 Protease-Activated Receptors in the Intestine: Focus on Inflammation and Cancer Sébert, Morgane Sola-Tapias, Nuria Mas, Emmanuel Barreau, Frédérick Ferrand, Audrey Front Endocrinol (Lausanne) Endocrinology Protease-activated receptors (PARs) belong to the G protein-coupled receptor (GPCR) family. Compared to other GPCRs, the specificity of the four PARs is the lack of physiologically soluble ligands able to induce their activation. 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 diseases and cancer. Frontiers Media S.A. 2019-10-24 /pmc/articles/PMC6821688/ /pubmed/31708870 http://dx.doi.org/10.3389/fendo.2019.00717 Text en Copyright © 2019 Sébert, Sola-Tapias, Mas, Barreau and Ferrand. http://creativecommons.org/licenses/by/4.0/ 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.
spellingShingle Endocrinology
Sébert, Morgane
Sola-Tapias, Nuria
Mas, Emmanuel
Barreau, Frédérick
Ferrand, Audrey
Protease-Activated Receptors in the Intestine: Focus on Inflammation and Cancer
title Protease-Activated Receptors in the Intestine: Focus on Inflammation and Cancer
title_full Protease-Activated Receptors in the Intestine: Focus on Inflammation and Cancer
title_fullStr Protease-Activated Receptors in the Intestine: Focus on Inflammation and Cancer
title_full_unstemmed Protease-Activated Receptors in the Intestine: Focus on Inflammation and Cancer
title_short Protease-Activated Receptors in the Intestine: Focus on Inflammation and Cancer
title_sort protease-activated receptors in the intestine: focus on inflammation and cancer
topic Endocrinology
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6821688/
https://www.ncbi.nlm.nih.gov/pubmed/31708870
http://dx.doi.org/10.3389/fendo.2019.00717
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