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Your search keyword '"Saied, Essa M."' showing total 4 results
Start Over Author "Saied, Essa M." Journal angewandte chemie
4 results on '"Saied, Essa M."'

1. 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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2. Innentitelbild: Unterscheidung von isomeren Sphingolipiden mittels kryogener Infrarotspektroskopie (Angew. Chem. 32/2020)

Author

Kirschbaum, Carla, primary, Saied, Essa M., additional, Greis, Kim, additional, Mucha, Eike, additional, Gewinner, Sandy, additional, Schöllkopf, Wieland, additional, Meijer, Gerard, additional, Helden, Gert, additional, Poad, Berwyck L. J., additional, Blanksby, Stephen J., additional, Arenz, Christoph, additional, and Pagel, Kevin, additional

Published
2020
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4. 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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