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
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Acceso en línea:https://doaj.org/article/a14531ed08b24689ae4bc18c982d5788
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