Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474

A recent phase 1 trial of the fatty acid amide hydrolase (FAAH) inhibitor BIA 10-2474 led to the death of one volunteer and produced mild-to-severe neurological symptoms in four others. Although the cause of the clinical neurotoxicity is unknown, it has been postulated, given the clinical safety pro...

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Veröffentlicht in:	Science (American Association for the Advancement of Science) Jg. 356; H. 6342; S. 1084
Hauptverfasser:	van Esbroeck, Annelot C M, Janssen, Antonius P A, Cognetta, 3rd, Armand B, Ogasawara, Daisuke, Shpak, Guy, van der Kroeg, Mark, Kantae, Vasudev, Baggelaar, Marc P, de Vrij, Femke M S, Deng, Hui, Allarà, Marco, Fezza, Filomena, Lin, Zhanmin, van der Wel, Tom, Soethoudt, Marjolein, Mock, Elliot D, den Dulk, Hans, Baak, Ilse L, Florea, Bogdan I, Hendriks, Giel, De Petrocellis, Luciano, Overkleeft, Herman S, Hankemeier, Thomas, De Zeeuw, Chris I, Di Marzo, Vincenzo, Maccarrone, Mauro, Cravatt, Benjamin F, Kushner, Steven A, van der Stelt, Mario
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	United States 09.06.2017
Schlagworte:	Amidohydrolases - antagonists & inhibitors Analgesics - adverse effects Analgesics - chemistry Analgesics - metabolism Analgesics - pharmacology Anti-Anxiety Agents - adverse effects Anti-Anxiety Agents - chemistry Anti-Anxiety Agents - metabolism Anti-Anxiety Agents - pharmacology Cell Line, Tumor Clinical Trials, Phase I as Topic Cross Reactions Cyclic N-Oxides - adverse effects Cyclic N-Oxides - chemistry Cyclic N-Oxides - metabolism Cyclic N-Oxides - pharmacology Humans Neurons - drug effects Neurons - metabolism Protein Interaction Maps Pyridazines - pharmacology Pyridazines - therapeutic use Pyridines - adverse effects Pyridines - chemistry Pyridines - metabolism Pyridines - pharmacology Urea - analogs & derivatives Urea - pharmacology Urea - therapeutic use
ISSN:	1095-9203, 1095-9203
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