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.

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Autores principales:	Anne-Marinette Cao, Robert B. Quast, Fataneh Fatemi, Philippe Rondard, Jean-Philippe Pin, Emmanuel Margeat
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/a14531ed08b24689ae4bc18c982d5788
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spelling	oai:doaj.org-article:a14531ed08b24689ae4bc18c982d57882021-12-02T15:16:10ZAllosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state10.1038/s41467-021-25620-52041-1723https://doaj.org/article/a14531ed08b24689ae4bc18c982d57882021-09-01T00:00:00Zhttps://doi.org/10.1038/s41467-021-25620-5https://doaj.org/toc/2041-1723Here, 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.Anne-Marinette CaoRobert B. QuastFataneh FatemiPhilippe RondardJean-Philippe PinEmmanuel MargeatNature PortfolioarticleScienceQENNature Communications, Vol 12, Iss 1, Pp 1-13 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q 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
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.
format	article
author	Anne-Marinette Cao Robert B. Quast Fataneh Fatemi Philippe Rondard Jean-Philippe Pin Emmanuel Margeat
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 Portfolio
publishDate	2021
url	https://doaj.org/article/a14531ed08b24689ae4bc18c982d5788
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Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state

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