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Hemorphins Targeting G Protein-Coupled Receptors

Hemorphins are short peptides produced by the proteolysis of the beta subunit of hemoglobin. These peptides have diverse physiological effects especially in the nervous and the renin-angiotensin systems. Such effects occur through the modulation of a diverse range of proteins including enzymes and r...

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Autores principales: Ayoub, Mohammed Akli, Vijayan, Ranjit
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7998264/
https://www.ncbi.nlm.nih.gov/pubmed/33799973
http://dx.doi.org/10.3390/ph14030225
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author Ayoub, Mohammed Akli
Vijayan, Ranjit
author_facet Ayoub, Mohammed Akli
Vijayan, Ranjit
author_sort Ayoub, Mohammed Akli
collection PubMed
description Hemorphins are short peptides produced by the proteolysis of the beta subunit of hemoglobin. These peptides have diverse physiological effects especially in the nervous and the renin-angiotensin systems. Such effects occur through the modulation of a diverse range of proteins including enzymes and receptors. In this review, we focus on pharmacological and functional targeting of G protein-coupled receptors (GPCRs) by hemorphins and their implication in physiology and pathophysiology. Among GPCRs, the opioid receptors constitute the first set of targets of hemorphins with implication in analgesia. Subsequently, several other GPCRs have been reported to be directly or indirectly involved in hemorphins’ action. This includes the receptors for angiotensin II, oxytocin, bombesin, and bradykinin, as well as the human MAS-related G protein-coupled receptor X1. Interestingly, both orthosteric activation and allosteric modulation of GPCRs by hemorphins have been reported. This review links hemorphins with GPCR pharmacology and signaling, supporting the implication of GPCRs in hemorphins’ effects. Thus, this aids a better understanding of the molecular basis of the action of hemorphins and further demonstrates that hemorphin-GPCR axis constitutes a valid target for therapeutic intervention in different systems.
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spelling pubmed-79982642021-03-28 Hemorphins Targeting G Protein-Coupled Receptors Ayoub, Mohammed Akli Vijayan, Ranjit Pharmaceuticals (Basel) Review Hemorphins are short peptides produced by the proteolysis of the beta subunit of hemoglobin. These peptides have diverse physiological effects especially in the nervous and the renin-angiotensin systems. Such effects occur through the modulation of a diverse range of proteins including enzymes and receptors. In this review, we focus on pharmacological and functional targeting of G protein-coupled receptors (GPCRs) by hemorphins and their implication in physiology and pathophysiology. Among GPCRs, the opioid receptors constitute the first set of targets of hemorphins with implication in analgesia. Subsequently, several other GPCRs have been reported to be directly or indirectly involved in hemorphins’ action. This includes the receptors for angiotensin II, oxytocin, bombesin, and bradykinin, as well as the human MAS-related G protein-coupled receptor X1. Interestingly, both orthosteric activation and allosteric modulation of GPCRs by hemorphins have been reported. This review links hemorphins with GPCR pharmacology and signaling, supporting the implication of GPCRs in hemorphins’ effects. Thus, this aids a better understanding of the molecular basis of the action of hemorphins and further demonstrates that hemorphin-GPCR axis constitutes a valid target for therapeutic intervention in different systems. MDPI 2021-03-07 /pmc/articles/PMC7998264/ /pubmed/33799973 http://dx.doi.org/10.3390/ph14030225 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ).
spellingShingle Review
Ayoub, Mohammed Akli
Vijayan, Ranjit
Hemorphins Targeting G Protein-Coupled Receptors
title Hemorphins Targeting G Protein-Coupled Receptors
title_full Hemorphins Targeting G Protein-Coupled Receptors
title_fullStr Hemorphins Targeting G Protein-Coupled Receptors
title_full_unstemmed Hemorphins Targeting G Protein-Coupled Receptors
title_short Hemorphins Targeting G Protein-Coupled Receptors
title_sort hemorphins targeting g protein-coupled receptors
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7998264/
https://www.ncbi.nlm.nih.gov/pubmed/33799973
http://dx.doi.org/10.3390/ph14030225
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