Ontology highlight
ABSTRACT:
SUBMITTER: Sugasawa Y
PROVIDER: S-EPMC7532004 | biostudies-literature | 2020 Sep
REPOSITORIES: biostudies-literature
Sugasawa Yusuke Y Cheng Wayland Wl WW Bracamontes John R JR Chen Zi-Wei ZW Wang Lei L Germann Allison L AL Pierce Spencer R SR Senneff Thomas C TC Krishnan Kathiresan K Reichert David E DE Covey Douglas F DF Akk Gustav G Evers Alex S AS
eLife 20200921
This study examines how site-specific binding to three identified neurosteroid-binding sites in the α<sub>1</sub>β<sub>3</sub> GABA<sub>A</sub> receptor (GABA<sub>A</sub>R) contributes to neurosteroid allosteric modulation. We found that the potentiating neurosteroid, allopregnanolone, but not its inhibitory 3β-epimer epi-allopregnanolone, binds to the canonical β<sub>3</sub>(+)-α<sub>1</sub>(-) intersubunit site that mediates receptor activation by neurosteroids. In contrast, both allopregnanol ...[more]