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An original potentiating mechanism revealed by the cryo-EM structures of the human α7 nicotinic receptor in complex with nanobodies

The α7 nicotinic receptor mediates neuronal communication in the brain. Here, the authors present cryo-EM structures of α7 in complex with single-chain antibodies, revealing an original mechanism of potentiation useful for the design of pro-cognitive drugs.

Marie S. Prevost
Nathalie Barilone
Pierre-Jean Corringer
ResearchOpen Access25 Sept 2023
Nature Communications

Volume: 14, P: 1-13
Illumination of a progressive allosteric mechanism mediating the glycine receptor activation

Glycine receptors are channel receptors mediating signal transduction between neurons that transit between resting and open states upon neurotransmitter binding. Here, the authors illuminate a progressive transition of opening by combining voltage-clamp fluorometry and molecular dynamics.

Sophie Shi
Solène N. Lefebvre
Pierre-Jean Corringer
ResearchOpen Access13 Feb 2023
Nature Communications

Volume: 14, P: 1-13
X-ray structure of a pentameric ligand-gated ion channel in an apparently open conformation

Recently, the first crystal structure of a pentameric ligand-gated ion channel known as GLIC was published, which represented a closed state of the channel. In two papers in this issue, presumptive open states of a related channel — ELIC — have been crystallized and show significant tilting of the M2 and M3 α-helices from the closed state.

Nicolas Bocquet
Hugues Nury
Pierre-Jean Corringer
Research05 Nov 2008
Nature

Volume: 457, P: 111-114
A prokaryotic proton-gated ion channel from the nicotinic acetylcholine receptor family

Nicolas Bocquet
Lia Prado de Carvalho
Pierre-Jean Corringer
Research10 Dec 2006
Nature

Volume: 445, P: 116-119
A millisecond coarse-grained simulation approach to decipher allosteric cannabinoid binding at the glycine receptor α1

Cannabinoids potentiate responses of brain receptors, but their mechanism of action is unknown. Here, using coarse-grained MD simulations and electrophysiology of mutants, the authors elucidate the allosteric binding sites for two cannabinoids at the glycine receptor.

Alessio Bartocci
Andrea Grazzi
Marco Cecchini
ResearchOpen Access19 Oct 2024
Nature Communications

Volume: 15, P: 1-13
The desensitization pathway of GABA_A receptors, one subunit at a time

GABA_A receptors mediate most inhibitory synaptic transmission in the brain. Here authors used concatemeric α1β2γ2 GABA_A receptors to introduce gain-of-desensitization mutations one subunit at a time, revealing non-concerted rearrangements with a key contribution of the γ2 subunit during desensitization.

Marc Gielen
Nathalie Barilone
Pierre-Jean Corringer
ResearchOpen Access23 Oct 2020
Nature Communications

Volume: 11, P: 1-14
Structural basis for potentiation by alcohols and anaesthetics in a ligand-gated ion channel

Alcohols and anaesthetics exert their effects by potentiating ligand-gated ion channels. Here, the authors determine crystal structures of a bacterial ligand-gated ion channel in the presence of alcohols and anaesthetics, and describe a structural mechanism for stabilization of the open form of the channel.

Ludovic Sauguet
Rebecca J. Howard
Marc Delarue
Research16 Apr 2013
Nature Communications

Volume: 4, P: 1-10
A locally closed conformation of a bacterial pentameric proton-gated ion channel

Pentameric ligand-gated ion channels (pLGICs) mediate fast synaptic signaling in response to neurotransmitter binding, but the conformational changes induced by neurotransmitter binding are unknown. The crystal structures of mutated GLIC, a bacterial pLGIC homolog, reveal a novel, locally closed channel conformation that provides insight into pLGIC allosteric transitions.

Marie S Prevost
Ludovic Sauguet
Pierre-Jean Corringer
Research13 May 2012
Nature Structural & Molecular Biology

Volume: 19, P: 642-649
Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system

The nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels, the activity of which modulates many neurotransmitter systems. They are therefore therapeutic targets for the treatment of several central nervous system disorders. In this article, Taly and colleagues present recent advances in our understanding of the atomic structure, functional organization and conformational transitions of the nAChR that may be applied to drug discovery, and discuss agents currently in development.

Antoine Taly
Pierre-Jean Corringer
Jean-Pierre Changeux
Reviews01 Sept 2009
Nature Reviews Drug Discovery

Volume: 8, P: 733-750
Conformational transitions of the serotonin 5-HT₃ receptor

Cryo-electron microscopy of the serotonin 5-HT3 receptor in complex with various ligands yields four distinct structures, capturing serotonin binding in detail and increasing understanding of the gating mechanism of the receptor.

Lucie Polovinkin
Ghérici Hassaine
Hugues Nury
Research31 Oct 2018
Nature

Volume: 563, P: 275-279
X-ray structures of general anaesthetics bound to a pentameric ligand-gated ion channel

The mechanism of action of general anaesthetics is poorly understood, although there is some evidence that their principal protein targets are pentameric ligand-gated ion channels (pLGICs). Here, the X-ray crystal structures of propofol and desflurane bound to a bacterial homologue of the pLGIC family are solved. The structures reveal a common binding site for these two anaesthetics in the upper part of the transmembrane domain of each protomer.

Hugues Nury
Catherine Van Renterghem
Pierre-Jean Corringer
Research19 Jan 2011
Nature

Volume: 469, P: 428-431
Modulation of glycine receptor single-channel conductance by intracellular phosphorylation

Gustavo Moraga-Cid
Victoria P. San Martín
Gonzalo E. Yévenes
ResearchOpen Access16 Mar 2020
Scientific Reports

Volume: 10, P: 1-11
Interaction of Synthetic Human SLURP-1 with the Nicotinic Acetylcholine Receptors

Thomas Durek
Irina V. Shelukhina
Victor I. Tsetlin
ResearchOpen Access30 Nov 2017
Scientific Reports

Volume: 7, P: 1-11
Smoke Extracts and Nicotine, but not Tobacco Extracts, Potentiate Firing and Burst Activity of Ventral Tegmental Area Dopaminergic Neurons in Mice

Fabio Marti
Ouafa Arib
Philippe Faure
Research29 Jun 2011
Neuropsychopharmacology

Volume: 36, P: 2244-2257

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