GABAA receptor proline 273 at the interdomain interface of the β2 subunit regulates entry into desensitization and opening/closing transitions
Life Sciences(2022)
Abstract
In conclusion, we demonstrate that βP273 of the M2-M3 linker is a crucial element of the ECD-TMD interface regulating the receptor's ability to undergo late gating transitions. Henceforth, this region could be an important target for new pharmacological tools affecting GABAR-mediated inhibition.
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Key words
Gamma-aminobutyric acid,Pentameric ligand-gated ion channels,Gating,Desensitization,Structure-function relationship
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