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PDBsum entry 6d6t
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Transport protein
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PDB id
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6d6t
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Contents |
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333 a.a.
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333 a.a.
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302 a.a.
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106 a.a.
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116 a.a.
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References listed in PDB file
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Key reference
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Title
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Structure of a human synaptic gabaa receptor.
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Authors
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S.Zhu,
C.M.Noviello,
J.Teng,
R.M.Walsh,
J.J.Kim,
R.E.Hibbs.
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Ref.
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Nature, 2018,
559,
67-72.
[DOI no: ]
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PubMed id
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Abstract
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Fast inhibitory neurotransmission in the brain is principally mediated by the
neurotransmitter GABA (γ-aminobutyric acid) and its synaptic target, the type A
GABA receptor (GABAA receptor). Dysfunction of this receptor results
in neurological disorders and mental illnesses including epilepsy, anxiety and
insomnia. The GABAA receptor is also a prolific target for
therapeutic, illicit and recreational drugs, including benzodiazepines,
barbiturates, anaesthetics and ethanol. Here we present high-resolution
cryo-electron microscopy structures of the human α1β2γ2 GABAA
receptor, the predominant isoform in the adult brain, in complex with GABA and
the benzodiazepine site antagonist flumazenil, the first-line clinical treatment
for benzodiazepine overdose. The receptor architecture reveals unique
heteromeric interactions for this important class of inhibitory neurotransmitter
receptor. This work provides a template for understanding receptor modulation by
GABA and benzodiazepines, and will assist rational approaches to therapeutic
targeting of this receptor for neurological disorders and mental illness.
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