The five dimensions of receptor pharmacology exemplified by melatonin receptors: An opinion

Abstract Receptology has been complicated with enhancements in our knowledge of G‐protein‐coupled‐receptor (GPCR) biochemistry. This complexity is exemplified by the pharmacology of melatonin receptors. Here, we describe the complexity of GPCR biochemistry in five dimensions: (a) receptor expression...

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Main Authors: Jean A. Boutin, Céline Legros
Format: Article
Language:English
Published: Wiley 2020-02-01
Series:Pharmacology Research & Perspectives
Subjects:
Online Access:https://doi.org/10.1002/prp2.556
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spelling doaj-79c59ac6169e44b39512559e491472d62021-05-02T02:45:56ZengWileyPharmacology Research & Perspectives2052-17072020-02-0181n/an/a10.1002/prp2.556The five dimensions of receptor pharmacology exemplified by melatonin receptors: An opinionJean A. Boutin0Céline Legros1Institut de Recherches Internationales Servier Suresnes FranceInstitut de Recherches Servier Croissy‐sur‐Seine FranceAbstract Receptology has been complicated with enhancements in our knowledge of G‐protein‐coupled‐receptor (GPCR) biochemistry. This complexity is exemplified by the pharmacology of melatonin receptors. Here, we describe the complexity of GPCR biochemistry in five dimensions: (a) receptor expression, particularly in organs/tissues that are only partially understood; (b) ligands and receptor‐associated proteins (interactome); (c) receptor function, which might be more complex than the known G‐protein‐coupled systems; (d) ligand bias, which favors a particular pathway; and (e) receptor dimerization, which might concern all receptors coexpressed in the same cell. Thus, receptor signaling might be modified or modulated, depending on the nature of the receptor complex. Fundamental studies are needed to clarify these points and find new ways to tackle receptor functionality. This opinion article emphasizes the global questions attached to new descriptions of GPCRs and aims to raise our awareness of the tremendous complexity of modern receptology.https://doi.org/10.1002/prp2.556antagonismbiased ligandsdimerizationexpressionGPCRsinteractome
collection DOAJ
language English
format Article
sources DOAJ
author Jean A. Boutin
Céline Legros
spellingShingle Jean A. Boutin
Céline Legros
The five dimensions of receptor pharmacology exemplified by melatonin receptors: An opinion
Pharmacology Research & Perspectives
antagonism
biased ligands
dimerization
expression
GPCRs
interactome
author_facet Jean A. Boutin
Céline Legros
author_sort Jean A. Boutin
title The five dimensions of receptor pharmacology exemplified by melatonin receptors: An opinion
title_short The five dimensions of receptor pharmacology exemplified by melatonin receptors: An opinion
title_full The five dimensions of receptor pharmacology exemplified by melatonin receptors: An opinion
title_fullStr The five dimensions of receptor pharmacology exemplified by melatonin receptors: An opinion
title_full_unstemmed The five dimensions of receptor pharmacology exemplified by melatonin receptors: An opinion
title_sort five dimensions of receptor pharmacology exemplified by melatonin receptors: an opinion
publisher Wiley
series Pharmacology Research & Perspectives
issn 2052-1707
publishDate 2020-02-01
description Abstract Receptology has been complicated with enhancements in our knowledge of G‐protein‐coupled‐receptor (GPCR) biochemistry. This complexity is exemplified by the pharmacology of melatonin receptors. Here, we describe the complexity of GPCR biochemistry in five dimensions: (a) receptor expression, particularly in organs/tissues that are only partially understood; (b) ligands and receptor‐associated proteins (interactome); (c) receptor function, which might be more complex than the known G‐protein‐coupled systems; (d) ligand bias, which favors a particular pathway; and (e) receptor dimerization, which might concern all receptors coexpressed in the same cell. Thus, receptor signaling might be modified or modulated, depending on the nature of the receptor complex. Fundamental studies are needed to clarify these points and find new ways to tackle receptor functionality. This opinion article emphasizes the global questions attached to new descriptions of GPCRs and aims to raise our awareness of the tremendous complexity of modern receptology.
topic antagonism
biased ligands
dimerization
expression
GPCRs
interactome
url https://doi.org/10.1002/prp2.556
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