Direct structural insights into GABAA receptor pharmacology

JJ Kim, RE Hibbs - Trends in biochemical sciences, 2021 - cell.com
GABA A receptors are pentameric ligand-gated ion channels that mediate most fast
neuronal inhibition in the brain. In addition to their important physiological roles, they are …

Cryo-electron microscopy: moving beyond X-ray crystal structures for drug receptors and drug development

J García-Nafría, CG Tate - Annual review of pharmacology and …, 2020 - annualreviews.org
Electron cryo-microscopy (cryo-EM) has revolutionized structure determination of membrane
proteins and holds great potential for structure-based drug discovery. Here we discuss the …

GABAA receptor signalling mechanisms revealed by structural pharmacology

S Masiulis, R Desai, T Uchański, I Serna Martin… - Nature, 2019 - nature.com
Type-A γ-aminobutyric (GABAA) receptors are ligand-gated chloride channels with a very
rich pharmacology. Some of their modulators, including benzodiazepines and general …

Architecture and assembly mechanism of native glycine receptors

H Zhu, E Gouaux - Nature, 2021 - nature.com
Glycine receptors (GlyRs) are pentameric,'Cys-loop'receptors that form chloride-permeable
channels and mediate fast inhibitory signalling throughout the central nervous system,. In …

Mesophasic organization of GABAA receptors in hippocampal inhibitory synapses

YT Liu, CL Tao, X Zhang, W **a, DQ Shi, L Qi… - Nature …, 2020 - nature.com
Abstract Information processing in the brain depends on specialized organization of
neurotransmitter receptors and scaffolding proteins within the postsynaptic density …

[HTML][HTML] Elephants in the dark: Insights and incongruities in pentameric ligand-gated ion channel models

RJ Howard - Journal of Molecular Biology, 2021 - Elsevier
The superfamily of pentameric ligand-gated ion channels (pLGICs) comprises key players in
electrochemical signal transduction across evolution, including historic model systems for …

Epiberberine induced p53/p21-dependent G2/M cell cycle arrest and cell apoptosis in gastric cancer cells by activating γ-aminobutyric acid receptor-β3

M Li, J Yang, J Li, Y Zhou, X Li, Z Ma, X Li, H Ma, X Ye - Phytomedicine, 2024 - Elsevier
Abstract Background and Purpose Epiberberine (EPI) is one of the most important
bioalkaloid found in the rhizome of Coptis chinensis, which has been observed to exhibit …

Neurosteroids and their potential as a safer class of general anesthetics

H Tateiwa, AS Evers - Journal of anesthesia, 2024 - Springer
Neurosteroids (NS) are a class of steroids that are synthesized within the central nervous
system (CNS). Various NS can either enhance or inhibit CNS excitability and they play …

Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies

LK Golani, MY Mian, T Ahmed, KP Pandey… - Bioorganic & Medicinal …, 2022 - Elsevier
The pharmacological actions exerted by benzodiazepines are dependent on the discrete α
protein subunits of the γ-aminobutyric acid type A receptor (GABA AR). Recent …

Identification of the initial steps in signal transduction in the α4β2 nicotinic receptor: insights from equilibrium and nonequilibrium simulations

ASF Oliveira, DK Shoemark, HR Campello… - Structure, 2019 - cell.com
Nicotinic acetylcholine receptors (nAChRs) modulate synaptic transmission in the nervous
system. These receptors have emerged as therapeutic targets in drug discovery for treating …