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.
| Main Authors: | , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Nature Publishing Group
2021-09-01
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| Series: | Nature Communications |
| Online Access: | https://doi.org/10.1038/s41467-021-25620-5 |