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Comment
. 2021 Jul;42(7):507-509.
doi: 10.1016/j.tips.2021.04.008. Epub 2021 May 6.

Partial agonists go molecular

Mark L Mayer  1
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Comment

Partial agonists go molecular

Mark L Mayer. Trends Pharmacol Sci. 2021 Jul.

Abstract

Single-channel analysis previously revealed a key role for a short-lived 'flipped' state during glycine receptor activation by partial agonists. Structures solved by Yu and colleagues now reveal a surprising mechanism involving a partially activated agonist-bound closed state that is too long-lived to be considered the flipped state.

Keywords: cryo-electron microscopy; glycine receptors; ligand-gated ion channels; single-channel recording.

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