The Binding of Palonosetron and Other Antiemetic Drugs to the Serotonin 5-HT3 Receptor

Autor: Guy Schoehn, Wensheng Cai, Jonathan Perot, Hugues Nury, François Dehez, Hong Zhang, Grégory Effantin, Christophe Chipot, Jacques Neyton, Eleftherios Zarkadas

Publikováno v: Structure
Structure, 2020, 28 (10), pp.1131-1140.e4. ⟨10.1016/j.str.2020.07.004⟩
Structure, Elsevier (Cell Press), 2020, 28 (10), pp.1131-1140.e4. ⟨10.1016/j.str.2020.07.004⟩

Inaccurately perceived as niche drugs, antiemetics are key elements of cancer treatment alleviating the most dreaded side effect of chemotherapy. Serotonin 5-HT3 receptor antagonists are the most commonly prescribed class of drugs to control chemothe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::93fdd42b49ef922fcc550bb0f0dd190a
https://hal.science/hal-03076599

Conformational transitions of the serotonin 5-HT

Autor: Lucie, Polovinkin, Ghérici, Hassaine, Jonathan, Perot, Emmanuelle, Neumann, Anders A, Jensen, Solène N, Lefebvre, Pierre-Jean, Corringer, Jacques, Neyton, Christophe, Chipot, Francois, Dehez, Guy, Schoehn, Hugues, Nury

Publikováno v: Nature. 563(7730)

The serotonin 5-HT3 receptor is a pentameric ligand-gated ion channel (pLGIC). It belongs to a large family of receptors that function as allosteric signal transducers across the plasma membrane(1,2): upon binding of neurotransmitter molecules to ext

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::4823e9dfeb4673fcd335d4a9df208ec0
https://pubmed.ncbi.nlm.nih.gov/30401839

Synthesis and Biological Evaluation of 1-Amino-2-Phosphonomethylcyclopropanecarboxylic Acids, New Group III Metabotropic Glutamate Receptor Agonists

Autor: Cyril Goudet, Hugues-Olivier Bertrand, Isabelle Brabet, Michael J. Marino, Pauline Sibille, Florence Gaven, Sébastien Lopez, Jacques Neyton, Jean-Philippe Pin, Ornella Valenti, Francine Acher, Nadia Oueslati, Marianne Amalric

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, American Chemical Society, 2007, 50 (15), pp.3585-95. ⟨10.1021/jm070262c⟩
Journal of Medicinal Chemistry, American Chemical Society, 2007, 50 (15), pp.3585-95. 〈10.1021/jm070262c〉
Journal of Medicinal Chemistry, 2007, 50 (15), pp.3585-95. ⟨10.1021/jm070262c⟩

International audience; Stereoisomers of 1-amino-2-phosphonomethylcyclopropanecarboxylic acid (APCPr), conformationally restricted analogues of L-AP4 (2-amino-4-phosphonobutyric acid), have been prepared and evaluated at recombinant group III metabot

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b1bd7047c1a9b87b58e5e71873c12613
https://doi.org/10.1021/jm070262c

A Startling Role for Synaptic Zinc

Autor: Pierre Paoletti, Jacques Neyton, Alan R. Kay

Publikováno v: Neuron
Neuron, Elsevier, 2006, 52 (4), pp.572-4. ⟨10.1016/j.neuron.2006.11.007⟩

It has long been known that the synaptic vesicles of certain glutamatergic terminals, as well as some inhibitory terminals, are richly supplied with zinc ions, yet the functional role of this pool of zinc in synaptic transmission has remained elusive

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d49b0908eeaa4c7a30cdef5d337312fa

Probing the pore region of recombinant N-methyl-D-aspartate channels using external and internal magnesium block

Autor: Jacques Neyton, P Ascher, Jurgen Kupper

Publikováno v: Proceedings of the National Academy of Sciences. 93:8648-8653

Mg2+ ions block N-methyl-D-aspartate (NMDA) channels by entering the pore from either the extracellular or the cytoplasmic side of the membrane in a voltage-dependent manner. We have used these two different block phenomena to probe the structure of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a519421e2b1f0739e79689b8a4e9196c
https://doi.org/10.1073/pnas.93.16.8648