Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state

Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state

Here, the authors use smFRET to assess the structural dynamics of metabotropic glutamate receptor mGlu2 and show that a positive allosteric modulator or the Gi protein stabilize mGlu2 in the glutamate-induced active state, leading to the full activation of the receptor.

Bibliographic Details
Main Authors: Anne-Marinette Cao, Robert B. Quast, Fataneh Fatemi, Philippe Rondard, Jean-Philippe Pin, Emmanuel Margeat
Format: Article
Language:English
Published: Nature Publishing Group 2021-09-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-021-25620-5
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spelling doaj-a14531ed08b24689ae4bc18c982d57882021-09-19T11:48:45ZengNature Publishing GroupNature Communications2041-17232021-09-0112111310.1038/s41467-021-25620-5Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active stateAnne-Marinette Cao0Robert B. Quast1Fataneh Fatemi2Philippe Rondard3Jean-Philippe Pin4Emmanuel Margeat5Centre de Biologie Structurale (CBS), Univ. Montpellier, CNRS, INSERMCentre de Biologie Structurale (CBS), Univ. Montpellier, CNRS, INSERMCentre de Biologie Structurale (CBS), Univ. Montpellier, CNRS, INSERMInstitut de Génomique Fonctionnelle, Univ. Montpellier, CNRS, INSERMInstitut de Génomique Fonctionnelle, Univ. Montpellier, CNRS, INSERMCentre de Biologie Structurale (CBS), Univ. Montpellier, CNRS, INSERMHere, the authors use smFRET to assess the structural dynamics of metabotropic glutamate receptor mGlu2 and show that a positive allosteric modulator or the Gi protein stabilize mGlu2 in the glutamate-induced active state, leading to the full activation of the receptor.https://doi.org/10.1038/s41467-021-25620-5
collection DOAJ
language English
format Article
sources DOAJ
author Anne-Marinette Cao
Robert B. Quast
Fataneh Fatemi
Philippe Rondard
Jean-Philippe Pin
Emmanuel Margeat
spellingShingle Anne-Marinette Cao
Robert B. Quast
Fataneh Fatemi
Philippe Rondard
Jean-Philippe Pin
Emmanuel Margeat
Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state
Nature Communications
author_facet Anne-Marinette Cao
Robert B. Quast
Fataneh Fatemi
Philippe Rondard
Jean-Philippe Pin
Emmanuel Margeat
author_sort Anne-Marinette Cao
title Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state
title_short Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state
title_full Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state
title_fullStr Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state
title_full_unstemmed Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state
title_sort allosteric modulators enhance agonist efficacy by increasing the residence time of a gpcr in the active state
publisher Nature Publishing Group
series Nature Communications
issn 2041-1723
publishDate 2021-09-01
description Here, the authors use smFRET to assess the structural dynamics of metabotropic glutamate receptor mGlu2 and show that a positive allosteric modulator or the Gi protein stabilize mGlu2 in the glutamate-induced active state, leading to the full activation of the receptor.
url https://doi.org/10.1038/s41467-021-25620-5
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