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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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PDB id:
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| Name: |
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Transport protein
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Title:
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Human gaba-a receptor alpha1-beta2-gamma2 subtype in complex with gaba and flumazenil, conformation b
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Structure:
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Gamma-aminobutyric acid receptor subunit beta-2,gamma- aminobutyric acid receptor subunit beta-2. Chain: a, c. Synonym: gaba(a) receptor subunit beta-2,gaba(a) receptor subunit beta-2. Engineered: yes. Gamma-aminobutyric acid receptor subunit alpha-1,gamma- aminobutyric acid receptor subunit alpha-1. Chain: b, d.
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Source:
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Homo sapiens. Human. Organism_taxid: 9606. Gene: gabrb2. Expressed in: homo sapiens. Expression_system_taxid: 9606. Expression_system_variant: gnti-. Expression_system_cell_line: hek293. Expression_system_atcc_number: crl-3022.
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Authors:
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S.Zhu,C.M.Noviello,J.Teng,R.M.Walsh Jr,J.J.Kim,R.E.Hibbs
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Key ref:
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S.Zhu
et al.
(2018).
Structure of a human synaptic GABAA receptor.
Nature,
559,
67-72.
PubMed id:
DOI:
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Date:
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22-Apr-18
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Release date:
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27-Jun-18
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PROCHECK
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Headers
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References
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P47870
(GBRB2_HUMAN) -
Gamma-aminobutyric acid receptor subunit beta-2 from Homo sapiens
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Seq:
Struc:
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512 a.a.
333 a.a.*
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P14867
(GBRA1_HUMAN) -
Gamma-aminobutyric acid receptor subunit alpha-1 from Homo sapiens
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Seq:
Struc:
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456 a.a.
333 a.a.*
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P18507
(GBRG2_HUMAN) -
Gamma-aminobutyric acid receptor subunit gamma-2 from Homo sapiens
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Seq:
Struc:
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475 a.a.
302 a.a.*
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DOI no:
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Nature
559:67-72
(2018)
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PubMed id:
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Structure of a human synaptic GABAA receptor.
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S.Zhu,
C.M.Noviello,
J.Teng,
R.M.Walsh,
J.J.Kim,
R.E.Hibbs.
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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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