The nicotinic acetylcholine receptor and its pentameric homologs: toward an allosteric mechanism of signal transduction at the atomic level

M Cecchini, PJ Corringer… - Annual Review of …, 2024 - annualreviews.org
The nicotinic acetylcholine receptor has served, since its biochemical identification in the
1970s, as a model of an allosteric ligand-gated ion channel mediating signal transition at the …

Agonist efficiency links binding and gating in a nicotinic receptor

DC Indurthi, A Auerbach - Elife, 2023 - elifesciences.org
Receptors signal by switching between resting (C) and active (O) shapes ('gating') under the
influence of agonists. The receptor's maximum response depends on the difference in …

Dynamics of receptor activation by agonists

A Auerbach - Biophysical Journal, 2024 - cell.com
How do agonists turn on receptors? The model system we have used to address this
question is the adult-type skeletal muscle nicotinic acetylcholine receptor. This ligand-gated …

Mechanisms underlying modulation of human GlyRα3 receptors by Zn2+ and pH

K Kindig, E Gibbs, D Seiferth, PC Biggin… - Science …, 2024 - science.org
Glycine receptors (GlyRs) regulate motor control and pain processing in the central nervous
system through inhibitory synaptic signaling. The subtype GlyRα3 expressed in nociceptive …

Exploring the Activation Process of the Glycine Receptor

J Yan, L Chen, A Warshel, C Bai - Journal of the American …, 2024 - ACS Publications
Glycine receptors (GlyR) conduct inhibitory glycinergic neurotransmission in the spinal cord
and the brainstem. They play an important role in muscle tone, motor coordination …

The effect of unliganded gating on agonist response in nicotinic receptors

DC Indurthi - European Journal of Pharmacology, 2024 - Elsevier
Understanding the agonist concentration-response curve (CRC) is the cornerstone in
pharmacology. While CRC parameters, agonist potency (EC 50) and efficacy (maximum …

Mapping the molecular motions of 5-HT3 serotonin-gated channel by Voltage-Clamp Fluorometry

L Peverini, S Shi, K Medjebeur, PJ Corringer - Elife, 2024 - elifesciences.org
The serotonin-gated ion channel (5-HT 3 R) mediates excitatory neuronal communication in
the gut and the brain. It is the target for setrons, a class of competitive antagonists widely …

变构蛋白的调控机制及其分子设计的研究进展.

曹伟洁, 陈林浩, 庞亚如, 成旭… - Chinese Journal of …, 2024 - search.ebscohost.com
变构蛋白是一类具有特殊变构效应的蛋白质, 其变构动态调节的多样性大大丰富了蛋白质的活性
或特异性. 探究蛋白变构效应及其调控机制, 在拓展蛋白功能, 药物研发和信号传递等方面具有 …

Asynchronous subunit transitions precede acetylcholine receptor activation

MJ Thompson, CJG Tessier, A Ananchenko, JR Emlaw… - bioRxiv, 2024 - biorxiv.org
Rapid communication at synapses is facilitated by postsynaptic receptors, which convert a
chemical signal into an electrical response. In the case of ligand-gated ion channels, agonist …

[PDF][PDF] Exploring Ligand Binding in Glycine-Gated Ion Channels with Molecular Dynamics and Enhanced Sampling Methods

J Clark - kclpure.kcl.ac.uk
To gain insights into the binding mechanism of glycine receptors, a range of approaches can
be employed including the utilisation of classical molecular dynamics and metadynamics …