α subunits in GABA_A receptors are dispensable for GABA and diazepam action.

ABSTRACT: The major isoform of the GABA_A receptor is α₁β₂γ₂. The binding sites for the agonist GABA are located at the β₂+/α₁- subunit interfaces and the modulatory site for benzodiazepines at α₁+/γ₂-. In the absence of α₁ subunits, a receptor was formed that was gated by GABA and modulated by diazepam similarly. This indicates that alternative subunits can take over the role of the α₁ subunits. Point mutations were introduced in β₂ or γ₂ subunits at positions homologous to α₁- benzodiazepine binding and GABA binding positions, respectively. From this mutation work we conclude that the site for GABA is located at a β₂+/β₂- subunit interf

SUBMITTER: Wongsamitkul N 

PROVIDER: S-EPMC5686171 | biostudies-literature | 2017 Nov

REPOSITORIES: biostudies-literature