Results 11 to 20 of about 8,951 (213)

Design of On-Target FAAH Inhibitors [PDF]

Chemistry & Biology, 2005
In this issue of Chemistry & Biology, Alexander and Cravatt propose a model for the binding of carbamate inhibitors to fatty acid amide hydrolase (FAAH), the enzyme that breaks down signaling lipids. Using competitive activity-based protein profiling and click chemistry, they designed potent and selective FAAH inhibitors and characterized their off ...
Deutsch, Dale G.
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The endocannabinoid hydrolase FAAH is an allosteric enzyme [PDF]

Scientific Reports, 2020
AbstractFatty acid amide hydrolase (FAAH) is a membrane-bound homodimeric enzyme that in vivo controls content and biological activity of N-arachidonoylethanolamine (AEA) and other relevant bioactive lipids termed endocannabinoids. Parallel orientation of FAAH monomers likely allows both subunits to simultaneously recruit and cleave substrates.
Dainese E., Oddi S., Simonetti M., Sabatucci A., Angelucci C. B., Ballone A., Dufrusine B., Fezza F., De Fabritiis G., Maccarrone M.   +9 more
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FAAH inhibitors in the limelight, but regrettably [PDF]

Int. Journal of Clinical Pharmacology and Therapeutics, 2016
This short review focuses on the recent drug development of FAAH inhibitors, as recent serious adverse events have been reported in a phase I study with a compound of this class. The authors overview the potential interest in targeting FAAH inhibition, the current programs, and the available information on the recent dramatic events.
Mallet, Christophe, Dubray, Claude, Dualé, Christian   +2 more
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Fluorimetric Assay of FAAH Activity

, 2022
Fatty acid amide hydrolase (FAAH) is the enzyme responsible for the degradation of anandamide (N-arachidonoylethanolamine, AEA) to arachidonic acid (AA) and ethanolamine. The method described here measures FAAH activity through the fluorometric arachidonoyl-7-amino-4-methyl-coumarin amide (AAMCA) substrate, which allows a simple and sensitive assay ...
Angelucci, Clotilde B, Giacominelli-Stuffler, Roberto, Maccarrone, Mauro   +2 more
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Radiometric Assay of FAAH Activity

, 2022
Fatty acid amide hydrolase (FAAH) is an intracellular enzyme responsible for the hydrolysis of endogenous anandamide (AEA), a reaction that terminates the biological effects of this lipid mediator. The final products of AEA cleavage are arachidonic acid and ethanolamine.
Bari, Monica, Feole, Monica, Fava, Marina, Maccarrone, Mauro   +3 more
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CRISPR interference at the FAAH-OUT genomic region reduces FAAH expression [PDF]

, 2019
Abstract FAAH-OUT encodes a putative long non-coding RNA which is located next to the FAAH gene on human chromosome 1. Recently an ~8 kb microdeletion, that removes upstream regulatory elements and the first 2 exons of FAAH-OUT ,
Mikaeili, Hajar, Yeung, Charlix, Habib, Abdella M, Wood, John N, Okorokov, Andrei L, Cox, James J   +5 more
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Membrane lipids are key modulators of the endocannabinoid-hydrolase FAAH

Biochemical Journal, 2014
Lipid composition is expected to play an important role in modulating membrane enzyme activity, in particular if the substrates are themselves lipid molecules. A paradigmatic case is FAAH (fatty acid amide hydrolase), an enzyme critical in terminating endocannabinoid signalling and an important therapeutic target. In the present study, using a combined
DAINESE, Enrico, De Fabritiis G, SABATUCCI, Annalaura, ODDI, Sergio, ANGELUCCI, Clotilde, Di Pancrazio C, Giorgino T, Stanley N, DEL CARLO, MICHELE, Cravatt B, Maccarrone M.   +10 more
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Role of FAAH-like anandamide transporter in anandamide inactivation.

PLoS ONE, 2013
The endocannabinoid system modulates numerous physiological processes including nociception and reproduction. Anandamide (AEA) is an endocannabinoid that is inactivated by cellular uptake followed by intracellular hydrolysis by fatty acid amide hydrolase
Kwannok Leung, Matthew W Elmes, Sherrye T Glaser, Dale G Deutsch, Martin Kaczocha   +4 more
doaj   +2 more sources

Just add water: cannabinoid discrimination in a water T-maze with FAAH(−/−) and FAAH(+/+) mice [PDF]

Behavioural Pharmacology, 2016
Incomplete overlap in the discriminative stimulus effects of Δ9-tetrahydrocannabinol (THC) and the endocannabinoids, anandamide (AEA) and 2-arachidonoylglycerol has been reported in food-reinforced tasks. The aim of this study was to examine cannabinoid discriminative stimulus effects in a nonappetitive procedure.
Jenny L, Wiley, Timothy W, Lefever, Nikita S, Pulley, Julie A, Marusich, Benjamin F, Cravatt, Aron H, Lichtman   +5 more
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FAAH-4 is involved in cholesterol mobilization by 2-AG.

, 2022
(A) Wild type and faah-4 animals grown for two generations in the absence of cholesterol at 20°C arrest as L2*. Feeding with 2-AG (50 μg/ml) increases the formation of adults in faah-4 animals compared with N2 animals.
Cecilia Vranych (14076749), Bruno Hernandez-Cravero (14076740), Sofia Gallino (14076743), Jeremy Florman (14076746), Philippe Diaz (1352535), Ana Belén Elgoyhen (14076752), Diego de Mendoza (9693935), Mark J. Alkema (8487948)   +7 more
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