Wird geladen...

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...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: Mileni, Mauro, Garfunkle, Joie, Ezzili, Cyrine, Cravatt, Benjamin F., Stevens, Raymond C., Boger, Dale L.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2011
Schlagworte:
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
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!