Binding and Inactivation Mechanism of a Humanized Fatty Acid Amide Hydrolase by α-Ketoheterocycle Inhibitors Revealed from Co-Crystal Structures

The co-crystal X-ray structures of two isomeric α-ketooxazole inhibitors (1 (OL-135) and 2) bound to fatty acid amide hydrolase (FAAH), a key enzymatic regulator of endocannabinoid signaling, are disclosed. The active site catalytic Ser241 is covalently bound to the inhibitors’ electrophilic carbony...

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Bibliografiska uppgifter
Huvudupphovsmän: Mileni, Mauro, Garfunkle, Joie, DeMartino, Jessica K., Cravatt, Benjamin F., Boger, Dale L., Stevens, Raymond C.
Materialtyp: Artigo
Språk:Inglês
Publicerad: 2009
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Article
Länkar:https://ncbi.nlm.nih.gov/pmc/articles/PMC2739126/
https://ncbi.nlm.nih.gov/pubmed/19722626
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ja902694n
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