Mechanism of partial agonism in AMPA-type glutamate receptors

Partial agonists weakly activate receptors even when occupying all available binding sites. Here the authors show that partial agonists of the AMPA receptor drive the adoption of multiple inactive forms, accounting for their limited efficacy.

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Auteurs principaux: Hector Salazar, Clarissa Eibl, Miriam Chebli, Andrew Plested
Format: article
Langue:EN
Publié: Nature Portfolio 2017
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Accès en ligne:https://doaj.org/article/299882cd5dc14ccfb46ea49f3ccbb9ae
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spelling oai:doaj.org-article:299882cd5dc14ccfb46ea49f3ccbb9ae2021-12-02T14:42:10ZMechanism of partial agonism in AMPA-type glutamate receptors10.1038/ncomms143272041-1723https://doaj.org/article/299882cd5dc14ccfb46ea49f3ccbb9ae2017-02-01T00:00:00Zhttps://doi.org/10.1038/ncomms14327https://doaj.org/toc/2041-1723Partial agonists weakly activate receptors even when occupying all available binding sites. Here the authors show that partial agonists of the AMPA receptor drive the adoption of multiple inactive forms, accounting for their limited efficacy.Hector SalazarClarissa EiblMiriam ChebliAndrew PlestedNature PortfolioarticleScienceQENNature Communications, Vol 8, Iss 1, Pp 1-11 (2017)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
Hector Salazar
Clarissa Eibl
Miriam Chebli
Andrew Plested
Mechanism of partial agonism in AMPA-type glutamate receptors
description Partial agonists weakly activate receptors even when occupying all available binding sites. Here the authors show that partial agonists of the AMPA receptor drive the adoption of multiple inactive forms, accounting for their limited efficacy.
format article
author Hector Salazar
Clarissa Eibl
Miriam Chebli
Andrew Plested
author_facet Hector Salazar
Clarissa Eibl
Miriam Chebli
Andrew Plested
author_sort Hector Salazar
title Mechanism of partial agonism in AMPA-type glutamate receptors
title_short Mechanism of partial agonism in AMPA-type glutamate receptors
title_full Mechanism of partial agonism in AMPA-type glutamate receptors
title_fullStr Mechanism of partial agonism in AMPA-type glutamate receptors
title_full_unstemmed Mechanism of partial agonism in AMPA-type glutamate receptors
title_sort mechanism of partial agonism in ampa-type glutamate receptors
publisher Nature Portfolio
publishDate 2017
url https://doaj.org/article/299882cd5dc14ccfb46ea49f3ccbb9ae
work_keys_str_mv AT hectorsalazar mechanismofpartialagonisminampatypeglutamatereceptors
AT clarissaeibl mechanismofpartialagonisminampatypeglutamatereceptors
AT miriamchebli mechanismofpartialagonisminampatypeglutamatereceptors
AT andrewplested mechanismofpartialagonisminampatypeglutamatereceptors
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