Target intelligence / Profile preview

Gamma-aminobutyric acid type A receptor subunit epsilon (GABRE)

Target
GABRE
Molecular classification
Ligand-gated ion channel, Ion channel, Receptor, Cys-loop receptor
01

Overview

Gamma-aminobutyric acid type A receptor subunit epsilon is a protein encoded by the GABRE gene and forms part of the heteropentameric GABA_A receptor, a chloride-selective ligand-gated ion channel that is critical for inhibitory synaptic transmission in the brain. The epsilon subunit contributes to the structural and functional heterogeneity of GABA_A receptors, which allow rapid hyperpolarization of neurons upon activation by GABA, the major inhibitory neurotransmitter. This subunit is primarily expressed in the brain but has been noted to participate in modulation of cardiac function as well. Variants in GABRE are associated with certain neuropsychiatric disorders, and the receptor as a whole is a major pharmacological target for diverse drug classes including anesthetics, benzodiazepines, and barbiturates.

Other names
GABREGamma-aminobutyric acid receptor subunit epsilonGABAAR subunit epsilonGABA(A) receptor subunit epsilonGABA(A) receptor, epsilongamma-aminobutyric acid (GABA) A receptor, epsilon subunitgamma-aminobutyric acid type A receptor epsilon subunit
02

Mechanism of action

Positive allosteric modulation (benzodiazepines, barbiturates, some anesthetics); Direct agonism/activation (GABA, muscimol); Competitive antagonism (bicuculline)

03

Biological functions

Inhibitory synaptic transmissionChloride ion transportRegulation of neuronal excitabilitySynaptic assemblyModulation of cardiac function (probable)
04

Disease associations

EpilepsyAutism spectrum disorderNeurodevelopmental and psychiatric disorders (potential role)
05

Safety considerations

SedationRespiratory depressionTolerance and dependence (with chronic drug modulation)Potential for cognitive impairment and impaired motor function
06

Interacting drugs

Benzodiazepines

4 more in the full profile.

07

Biomarkers

Altered GABRE expression or mutations may serve as biomarkers for epilepsy or autism spectrum disorder

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