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10 results on '"Fontanel Simon"'

1. Structural characterization of the active and inactive conformations of the vasopressin V2 receptor using cryo-EM

Author

Fouillen Aurelien, Julien Bous, Orcel Helene, Trapani Stefano, Cong Xiaojing, Dimon Juliette, Fontanel Simon, Saint-Paul Julie, Lai-Kee-Him Josephine, Urbach Serge, Sounier Remy, Bron Patrick, Granier Sebastien, and Mouillac Bernard

Subjects
cryo-em, v2r, structure-based drug design, Microbiology, QR1-502, Physiology, QP1-981, Zoology, QL1-991
Published
2024
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3. Structure of the vasopressin hormone–V2 receptor–β-arrestin1 ternary complex

Author

Bous, Julien, primary, Fouillen, Aurélien, additional, Orcel, Hélène, additional, Trapani, Stefano, additional, Cong, Xiaojing, additional, Fontanel, Simon, additional, Saint-Paul, Julie, additional, Lai-Kee-Him, Joséphine, additional, Urbach, Serge, additional, Sibille, Nathalie, additional, Sounier, Rémy, additional, Granier, Sébastien, additional, Mouillac, Bernard, additional, and Bron, Patrick, additional

Published
2022
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4. Discovery and Mechanism of Action of Small Molecule Inhibitors of Ceramidases**

Author

Healey, Robert D., primary, Saied, Essa M., additional, Cong, Xiaojing, additional, Karsai, Gergely, additional, Gabellier, Ludovic, additional, Saint‐Paul, Julie, additional, Del Nero, Elise, additional, Jeannot, Sylvain, additional, Drapeau, Marion, additional, Fontanel, Simon, additional, Maurel, Damien, additional, Basu, Shibom, additional, Leyrat, Cedric, additional, Golebiowski, Jérôme, additional, Bossis, Guillaume, additional, Bechara, Cherine, additional, Hornemann, Thorsten, additional, Arenz, Christoph, additional, and Granier, Sebastien, additional

Published
2021
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5. Mechanisms of GPCR hijacking byStaphylococcus aureus

Author

Grison, Claire M., primary, Leyrat, Cédric, additional, Lambey, Paul, additional, Jeannot, Sylvain, additional, Del Nero, Elise, additional, Fontanel, Simon, additional, Peysson, Fanny, additional, Heuninck, Joyce, additional, Sounier, Rémy, additional, Durroux, Thierry, additional, Granier, Sébastien, additional, and Bechara, Cherine, additional

Published
2021
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6. Silicalites and Mesoporous Silica Nanoparticles for photodynamic therapy

Author

Hocine, Ouahiba, Gary-Bobo, Magali, Brevet, David, Maynadier, Marie, Fontanel, Simon, Raehm, Laurence, Richeter, Sébastien, Loock, Bernard, Couleaud, Pierre, Frochot, Céline, Charnay, Clarence, Derrien, Gaëlle, Smaïhi, Monique, Sahmoune, Amar, Morère, Alain, Maillard, Philippe, Garcia, Marcel, and Durand, Jean-Olivier

Published
2010
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7. Discovery and Mechanism of Action of Small Molecule Inhibitors of Ceramidases**.

Author

Healey, Robert D., Saied, Essa M., Cong, Xiaojing, Karsai, Gergely, Gabellier, Ludovic, Saint‐Paul, Julie, Del Nero, Elise, Jeannot, Sylvain, Drapeau, Marion, Fontanel, Simon, Maurel, Damien, Basu, Shibom, Leyrat, Cedric, Golebiowski, Jérôme, Bossis, Guillaume, Bechara, Cherine, Hornemann, Thorsten, Arenz, Christoph, and Granier, Sebastien

Subjects
SMALL molecules, AMIDASES, HUMAN physiology, MASS spectrometry, CERAMIDES, DRUG development
Abstract

Sphingolipid metabolism is tightly controlled by enzymes to regulate essential processes in human physiology. The central metabolite is ceramide, a pro‐apoptotic lipid catabolized by ceramidase enzymes to produce pro‐proliferative sphingosine‐1‐phosphate. Alkaline ceramidases are transmembrane enzymes that recently attracted attention for drug development in fatty liver diseases. However, due to their hydrophobic nature, no specific small molecule inhibitors have been reported. We present the discovery and mechanism of action of the first drug‐like inhibitors of alkaline ceramidase 3 (ACER3). In particular, we chemically engineered novel fluorescent ceramide substrates enabling screening of large compound libraries and characterized enzyme:inhibitor interactions using mass spectrometry and MD simulations. In addition to revealing a new paradigm for inhibition of lipid metabolising enzymes with non‐lipidic small molecules, our data lay the ground for targeting ACER3 in drug discovery efforts. [ABSTRACT FROM AUTHOR]

Published
2022
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