Modulation of the turkey β1-adrenergic receptor by membrane rafts: insight from molecular dynamics

G-protein coupled receptors are targets for ~70% of drugs. These receptors are responsible for signal transduction within a cell membrane (and further into the cell) and disruption to this signaling cascade is responsible for several non-infectious diseases. Membrane rafts exhibit significantly alte...

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Main Authors: Ghumman, Afshan, Robinson, David
Format: Article
Published: Wiley 2016
Online Access:https://eprints.nottingham.ac.uk/36524/
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author Ghumman, Afshan
Robinson, David
author_facet Ghumman, Afshan
Robinson, David
author_sort Ghumman, Afshan
building Nottingham Research Data Repository
collection Online Access
description G-protein coupled receptors are targets for ~70% of drugs. These receptors are responsible for signal transduction within a cell membrane (and further into the cell) and disruption to this signaling cascade is responsible for several non-infectious diseases. Membrane rafts exhibit significantly altered properties in comparison to fluid bilayers and as such may regulate certain GPCR’s, or be responsible for errors in signaling. Using molecular dynamics, we have investigated the conformations of the turkey β1-adrenergic receptor with and without an agonist in sphingolipid and cholesterol rich bilayers, typical of raft compositions, and compared these to cholesterol-poor bilayers. We find that the raft-like lipid bilayers are responsible for significantly altering the conformation of the receptor, even when an agonist is present.
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spelling nottingham-365242020-05-04T18:13:02Z https://eprints.nottingham.ac.uk/36524/ Modulation of the turkey β1-adrenergic receptor by membrane rafts: insight from molecular dynamics Ghumman, Afshan Robinson, David G-protein coupled receptors are targets for ~70% of drugs. These receptors are responsible for signal transduction within a cell membrane (and further into the cell) and disruption to this signaling cascade is responsible for several non-infectious diseases. Membrane rafts exhibit significantly altered properties in comparison to fluid bilayers and as such may regulate certain GPCR’s, or be responsible for errors in signaling. Using molecular dynamics, we have investigated the conformations of the turkey β1-adrenergic receptor with and without an agonist in sphingolipid and cholesterol rich bilayers, typical of raft compositions, and compared these to cholesterol-poor bilayers. We find that the raft-like lipid bilayers are responsible for significantly altering the conformation of the receptor, even when an agonist is present. Wiley 2016-09-08 Article PeerReviewed Ghumman, Afshan and Robinson, David (2016) Modulation of the turkey β1-adrenergic receptor by membrane rafts: insight from molecular dynamics. ChemistrySelect, 1 (14). pp. 4274-4276. ISSN 2365-6549 http://onlinelibrary.wiley.com/doi/10.1002/slct.201600849/abstract;jsessionid=E2A11EE4B26662EF19BAFB412FC1E462.f01t03 doi:10.1002/slct.20160084 doi:10.1002/slct.20160084
spellingShingle Ghumman, Afshan
Robinson, David
Modulation of the turkey β1-adrenergic receptor by membrane rafts: insight from molecular dynamics
title Modulation of the turkey β1-adrenergic receptor by membrane rafts: insight from molecular dynamics
title_full Modulation of the turkey β1-adrenergic receptor by membrane rafts: insight from molecular dynamics
title_fullStr Modulation of the turkey β1-adrenergic receptor by membrane rafts: insight from molecular dynamics
title_full_unstemmed Modulation of the turkey β1-adrenergic receptor by membrane rafts: insight from molecular dynamics
title_short Modulation of the turkey β1-adrenergic receptor by membrane rafts: insight from molecular dynamics
title_sort modulation of the turkey β1-adrenergic receptor by membrane rafts: insight from molecular dynamics
url https://eprints.nottingham.ac.uk/36524/
https://eprints.nottingham.ac.uk/36524/
https://eprints.nottingham.ac.uk/36524/