GABAA receptors: structure, function, pharmacology, and related disorders

A Ghit, D Assal, AS Al-Shami, DEE Hussein - Journal of Genetic …, 2021 - Springer
Background γ-Aminobutyric acid sub-type A receptors (GABAARs) are the most prominent
inhibitory neurotransmitter receptors in the CNS. They are a family of ligand-gated ion …

GABAA receptors and the diversity in their structure and pharmacology

HC Chua, M Chebib - Advances in pharmacology, 2017 - Elsevier
Abstract GABA A receptors (GABA A Rs) are a class of ligand-gated ion channels with high
physiological and therapeutic significance. In the brain, these pentameric receptors occur …

Lactate buildup at the site of chronic inflammation promotes disease by inducing CD4+ T cell metabolic rewiring

V Pucino, M Certo, V Bulusu, D Cucchi, K Goldmann… - Cell metabolism, 2019 - cell.com
Accumulation of lactate in the tissue microenvironment is a feature of both inflammatory
disease and cancer. Here, we assess the response of immune cells to lactate in the context …

Structural insights into opposing actions of neurosteroids on GABAA receptors

DH Legesse, C Fan, J Teng, Y Zhuang… - Nature …, 2023 - nature.com
Abstract γ-Aminobutyric acid type A (GABAA) receptors mediate fast inhibitory signaling in
the brain and are targets of numerous drugs and endogenous neurosteroids. A subset of …

Crystal structures of a GABAA-receptor chimera reveal new endogenous neurosteroid-binding sites

D Laverty, P Thomas, M Field, OJ Andersen… - Nature structural & …, 2017 - nature.com
Abstract γ-Aminobutyric acid receptors (GABAARs) are vital for controlling excitability in the
brain. This is emphasized by the numerous neuropsychiatric disorders that result from …

Structural basis for GABAA receptor potentiation by neurosteroids

PS Miller, S Scott, S Masiulis, L De Colibus… - Nature structural & …, 2017 - nature.com
Type A γ-aminobutyric acid receptors (GABAARs) are the principal mediators of inhibitory
neurotransmission in the human brain. Endogenous neurosteroids interact with GABAARs to …

GABA receptors: pharmacological potential and pitfalls

M Jazvinscak Jembrek, J Vlainic - Current pharmaceutical …, 2015 - ingentaconnect.com
Gamma-amino butyric acid (GABA), the major inhibitory neurotransmitter in the mammalian
central nervous system, plays a key role in the regulation of neuronal transmission …

[HTML][HTML] Molecular mechanisms of antiseizure drug activity at GABAA receptors

LJ Greenfield Jr - Seizure, 2013 - Elsevier
Abstract The GABA A receptor (GABA AR) is a major target of antiseizure drugs (ASDs). A
variety of agents that act at GABA A Rs s are used to terminate or prevent seizures. Many act …

[HTML][HTML] GABAA receptor-acting neurosteroids: a role in the development and regulation of the stress response

BG Gunn, L Cunningham, SG Mitchell… - Frontiers in …, 2015 - Elsevier
Regulation of hypothalamic–pituitary–adrenocortical (HPA) axis activity by stress is a
fundamental survival mechanism and HPA-dysfunction is implicated in psychiatric disorders …

Neurosteroids, stress and depression: potential therapeutic opportunities

CF Zorumski, SM Paul, Y Izumi, DF Covey… - Neuroscience & …, 2013 - Elsevier
Neurosteroids are potent and effective neuromodulators that are synthesized from
cholesterol in the brain. These agents and their synthetic derivatives influence the function of …