Fluoride-Mediated Capture of a Noncovalent Bound State of a Reversible Covalent Enzyme Inhibitor: X-ray Crystallographic Analysis of an Exceptionally Potent α-Ketoheterocycle Inhibitor of Fatty Acid Amide Hydrolase

Two cocrystal X-ray structures of the exceptionally potent α-ketoheterocycle inhibitor 1 (K(i) = 290 pM) bound to a humanized variant of rat fatty acid amide hydrolase (FAAH) are disclosed, representing noncovalently and covalently bound states of the same inhibitor with the enzyme. Key to securing...

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Hauptverfasser: Mileni, Mauro, Garfunkle, Joie, Ezzili, Cyrine, Cravatt, Benjamin F., Stevens, Raymond C., Boger, Dale L.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2011
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC3060301/
https://ncbi.nlm.nih.gov/pubmed/21355555
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ja110877y
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