Steven De Gieter, Casey I Gallagher ... Rouslan G Efremov
Cryo-EM structures of Cys-loop receptor Alpo4 from the thermophilic worm Alvinella pompejana show that a sterol derivative CHAPS binds in and outside of its orthosteric binding site and induces a quaternary twist.
Hsp47 positively regulates the functional surface expression of endogenous GABAA receptors and plays a critical and general role in the maturation of Cys-loop neuroreceptors.
Development of nanobodies against a model pentameric ligand-gated ion channel demonstrates they can be functionally active as negative or positive allosteric modulators and offers opportunities for future drug development.
Laurie Peverini, Sophie Shi ... Pierre-Jean Corringer
Conformational motions elicited by antagonists, partial agonists, and agonists in serotonin-gated ion channels 5-HT3AR progressively spread from the extracellular to the transmembrane domain.
Victoria Juskaite, David S Corcoran, Birgit Leitinger
Ligand binding induces DDR1 kinase activity through recruitment of DDR1 receptors into signalling clusters in which phosphorylation occurs across different dimers.
Structures of the death domain of the p75 neurotrophin receptor in complex with downstream effectors show how competitive protein-protein interactions orchestrate the hierarchical activation of downstream pathways in non-catalytic receptors.
Anaïs Menny, Solène N Lefebvre ... Pierre-Jean Corringer
Allosteric reorganizations of a bacterial channel receptor are mapped along the protein structure, using the site-directed bimane quenching fluorescence technique, through parallel real-time conformational and electrophysiological recordings.