A screen of pharmacologically active compounds to identify modulators of the Adgrg6/Gpr126 signalling pathway in zebrafish embryos

A Asad, NO Shahidan… - Basic & Clinical …, 2023 - Wiley Online Library
Adhesion G protein‐coupled receptors (GPCRs) are an underrepresented class of GPCRs
in drug discovery. We previously developed an in vivo drug screening pipeline to identify …

[HTML][HTML] Cryo-EM structures of prokaryotic ligand-gated ion channel GLIC provide insights into gating in a lipid environment

N Bharambe, Z Li, D Seiferth, AM Balakrishna… - Nature …, 2024 - nature.com
GLIC, a proton-activated prokaryotic ligand-gated ion channel, served as a model system for
understanding the eukaryotic counterparts due to their structural and functional similarities …

[PDF][PDF] Structural mechanisms of α7 nicotinic receptor allosteric modulation and activation

SM Burke, M Avstrikova, CM Noviello, N Mukhtasimova… - Cell, 2024 - cell.com
The α7 nicotinic acetylcholine receptor is a pentameric ligand-gated ion channel that plays
an important role in cholinergic signaling throughout the nervous system. Its unique …

Allosteric Cholesterol Site in Glycine Receptors Characterized through Molecular Simulations

F Jalalypour, RJ Howard, E Lindahl - The Journal of Physical …, 2024 - ACS Publications
Glycine receptors are pentameric ligand-gated ion channels that conduct chloride ions
across postsynaptic membranes to facilitate fast inhibitory neurotransmission. In addition to …

[HTML][HTML] Asymmetric gating of a human hetero-pentameric glycine receptor

X Liu, W Wang - Nature communications, 2023 - nature.com
Hetero-pentameric Cys-loop receptors constitute a major type of neurotransmitter receptors
that enable signal transmission and processing in the nervous system. Despite intense …

[HTML][HTML] Molecular Pharmacology of Gelsemium Alkaloids on Inhibitory Receptors

AM Marileo, CO Lara, A Sazo, OV Contreras… - International Journal of …, 2024 - mdpi.com
Indole alkaloids are the main bioactive molecules of the Gelsemium genus plants. Diverse
reports have shown the beneficial actions of Gelsemium alkaloids on the pathological states …

GABAA receptor subunit M2-M3 linkers have asymmetric roles in pore gating and diazepam modulation

JW Nors, Z Endres, MP Goldschen-Ohm - Biophysical Journal, 2024 - cell.com
Abstract GABA A receptors (GABA A Rs) are neurotransmitter-gated ion channels critical for
inhibitory synaptic transmission as well as the molecular target for benzodiazepines (BZDs) …

Asymmetric roles for M2-M3 linkers of specific GABAA receptor subunits in the intrinsic closed-open equilibrium and its modulation by the benzodiazepine diazepam

JW Nors, Z Endres, MP Goldschen-Ohm - bioRxiv, 2023 - biorxiv.org
GABAA receptors (GABAARs) are neurotransmitter-gated ion channels critical for inhibitory
synaptic transmission as well as the molecular target for benzodiazepines (BZDs), one of the …

Exploring the Influence of Pore Shape on Conductance and Permeation

D Seiferth, PC Biggin - bioRxiv, 2024 - biorxiv.org
There are increasing numbers of ion channel structures featuring heteromeric subunit
assembly, exemplified by synaptic α1βB Glycine and α4β2 Nicotinic receptors. These …