A5067223769- Nicotinic Acetylcholine Receptors Study
- Ion channel regulation and function
- Receptor Mechanisms and Signaling
- Neuroscience and Neuropharmacology Research
- Mitochondrial Function and Pathology
- Chemical Reactions and Isotopes
- ATP Synthase and ATPases Research
- Molecular Sensors and Ion Detection
- Photoreceptor and optogenetics research
- Metabolism and Genetic Disorders
- Electrochemical Analysis and Applications
- Neurotransmitter Receptor Influence on Behavior
- Neuroscience and Neural Engineering
- Lipid Membrane Structure and Behavior
- Neuroendocrine regulation and behavior
- Anesthesia and Sedative Agents
- bioluminescence and chemiluminescence research
- Analytical Chemistry and Sensors
- Advanced Electron Microscopy Techniques and Applications
- Computational Drug Discovery Methods
- Antimicrobial Peptides and Activities
- Mass Spectrometry Techniques and Applications
- Pharmacological Receptor Mechanisms and Effects
- Enzyme Structure and Function
- Graphene research and applications
Institut de Biologie Structurale
2016-2025
Université Grenoble Alpes
2008-2025
Commissariat à l'Énergie Atomique et aux Énergies Alternatives
2006-2025
Centre National de la Recherche Scientifique
2012-2025
CEA Grenoble
2006-2025
École Polytechnique Fédérale de Lausanne
2013
Institut Pasteur
2008-2012
Laboratoire de Recherche sur la Croissance Cellulaire, la Réparation et la Régénération Tissulaires
2011-2012
Architecture et Fonction des Macromolécules Biologiques
2012
Laboratoire de Biologie Physico-Chimique des Protéines Membranaires
2011
The oligomerization state of the ADP/ATP carrier is an important issue in understanding mechanism underlying nucleotide exchange across inner mitochondrial membrane. first high resolution structure obtained presence carboxyatractyloside revealed a large cavity formed within monomer which inhibitor strongly bound. Whereas protein-protein interactions implicated crystal form are not biologically relevant, new described herein, highlights favorable interactions. mediated by endogenous...
Recently discovered bacterial homologues of eukaryotic pentameric ligand-gated ion channels, such as the Gloeobacter violaceus receptor (GLIC), are increasingly used structural and functional models signal transduction in nervous system. Here we present a one-microsecond-long molecular dynamics simulation GLIC channel pH stimulated gating mechanism. The crystal structure obtained at acidic an open-channel form is equilibrated membrane environment then instantly set to neutral pH. shows...
GABA(A) receptors are pentameric ligand-gated ion channels involved in fast inhibitory neurotransmission and allosterically modulated by the anxiolytic, anticonvulsant, sedative-hypnotic benzodiazepines. Here we show that prokaryotic homolog ELIC also is activated GABA benzodiazepines with effects comparable to those at receptors. Crystal structures reveal important features of recognition indicate benzodiazepines, depending on their concentration, occupy two possible sites ELIC. An...
Bites by elapid snakes (e.g. cobras) can result in life-threatening paralysis caused venom neurotoxins blocking neuromuscular nicotinic acetylcholine receptors. Here, we determine the cryo-EM structure of muscle-type Torpedo receptor complex with ScNtx, a recombinant short-chain α-neurotoxin. ScNtx is pinched between loop C on principal subunit and unique hairpin F complementary subunit, thereby access to neurotransmitter binding site. adopts mode that tilted toward forming wider network...
Abstract Synaptic receptors respond to neurotransmitters by opening an ion channel across the post-synaptic membrane elicit a cellular response. Here we use recent Torpedo acetylcholine receptor structures and functional measurements delineate key feature underlying allosteric communication between agonist-binding extracellular channel-gating transmembrane domains. Extensive mutagenesis at this inter-domain interface re-affirms critical energetically coupled role for principal α subunit...
The multifactorial origin and neurochemistry of Alzheimer's disease (AD) call for the development multitarget treatment strategies. We report a first-in-class triple acting compound that targets serotonin type 6 3 receptors (5-HT-Rs) monoamine oxidase B (MAO-B) as an approach treating AD. key structural features required MAO-B inhibition 5-HT6R antagonism interaction with 5-HT3R were determined using molecular dynamic simulations cryo-electron microscopy, respectively. Bioavailable PZ-1922...
Insect GABAA receptors are critical insecticide targets, with all 21st-century commercial compounds acting through a single allosteric membrane site. Here we describe three ligand binding sites and the associated receptor conformations for honeybee RDL receptor, combining cryo-EM, electrophysiology molecular dynamics. First conservation of GABA site explains absence insect-selective orthosteric compounds. Second, classical modulation site, occupied here by abamectin, exists in closed-pore...