Studying GPCR/cAMP pharmacology from the perspective of cellular structure

Signal transduction via G-protein coupled receptors (GPCRs) relies upon the production of cAMP and other signaling cascades. A given receptor and agonist pair, produce multiple effects upon cellular physiology which can be opposite in different cell types. The production of variable cellular effect...

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Main Authors: Peter T Wright, Sophie eSchobesberger, Julia eGorelik
Format: Article
Language:English
Published: Frontiers Media S.A. 2015-07-01
Series:Frontiers in Pharmacology
Subjects:
Online Access:http://journal.frontiersin.org/Journal/10.3389/fphar.2015.00148/full
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author Peter T Wright
Sophie eSchobesberger
Julia eGorelik
author_facet Peter T Wright
Sophie eSchobesberger
Julia eGorelik
author_sort Peter T Wright
collection DOAJ
description Signal transduction via G-protein coupled receptors (GPCRs) relies upon the production of cAMP and other signaling cascades. A given receptor and agonist pair, produce multiple effects upon cellular physiology which can be opposite in different cell types. The production of variable cellular effects via the signaling of the same GPCR in different cell types is a result of signal organization in space and time (compartmentation). This organization is usually based upon the physical and chemical properties of the membranes in which the GPCRs reside and the repertoire of downstream effectors and co-factors that are available at that location. In this review we explore mechanisms of GPCR signal compartmentation and broadly review the state-of-the-art methodologies which can be utilized to study them. We provide a clear rationale for a ‘localized’ approach to the study of the pharmacology and physiology of GPCRs and particularly the secondary messenger cAMP.
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spelling doaj.art-daa3182198504bc3b4567dc7da06bbdc2022-12-21T18:54:13ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122015-07-01610.3389/fphar.2015.00148154493Studying GPCR/cAMP pharmacology from the perspective of cellular structurePeter T Wright0Sophie eSchobesberger1Julia eGorelik2Imperial College LondonImperial College LondonImperial College LondonSignal transduction via G-protein coupled receptors (GPCRs) relies upon the production of cAMP and other signaling cascades. A given receptor and agonist pair, produce multiple effects upon cellular physiology which can be opposite in different cell types. The production of variable cellular effects via the signaling of the same GPCR in different cell types is a result of signal organization in space and time (compartmentation). This organization is usually based upon the physical and chemical properties of the membranes in which the GPCRs reside and the repertoire of downstream effectors and co-factors that are available at that location. In this review we explore mechanisms of GPCR signal compartmentation and broadly review the state-of-the-art methodologies which can be utilized to study them. We provide a clear rationale for a ‘localized’ approach to the study of the pharmacology and physiology of GPCRs and particularly the secondary messenger cAMP.http://journal.frontiersin.org/Journal/10.3389/fphar.2015.00148/fullCaveolaelipid raftsGPCRscAMPFRET sensorsCompartmentation
spellingShingle Peter T Wright
Sophie eSchobesberger
Julia eGorelik
Studying GPCR/cAMP pharmacology from the perspective of cellular structure
Frontiers in Pharmacology
Caveolae
lipid rafts
GPCRs
cAMP
FRET sensors
Compartmentation
title Studying GPCR/cAMP pharmacology from the perspective of cellular structure
title_full Studying GPCR/cAMP pharmacology from the perspective of cellular structure
title_fullStr Studying GPCR/cAMP pharmacology from the perspective of cellular structure
title_full_unstemmed Studying GPCR/cAMP pharmacology from the perspective of cellular structure
title_short Studying GPCR/cAMP pharmacology from the perspective of cellular structure
title_sort studying gpcr camp pharmacology from the perspective of cellular structure
topic Caveolae
lipid rafts
GPCRs
cAMP
FRET sensors
Compartmentation
url http://journal.frontiersin.org/Journal/10.3389/fphar.2015.00148/full
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