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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...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Frontiers Media S.A.
2019
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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. |
format | Online Article Text |
id | pubmed-6821688 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | Frontiers Media S.A. |
record_format | MEDLINE/PubMed |
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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