scholarly journals Fatty acid amide hydrolase (FAAH) inhibitor PF-3845 reduces viability, migration and invasiveness of human colon adenocarcinoma Colo-205 cell line: an in vitro study

2017 ◽  
Vol 64 (3) ◽  
pp. 519-525 ◽  
Author(s):  
Andrzej Wasilewski ◽  
Urszula Krajewska ◽  
Katarzyna Owczarek ◽  
Urszula Lewandowska ◽  
Jakub Fichna
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Colon Adenocarcinoma ◽  
In Vitro Study ◽  
Human Colon ◽  
Amide Hydrolase ◽  
Human Colon Adenocarcinoma ◽  
Fatty Acid Amide

ω-Imidazolyl- and ω-Tetrazolylalkylcarbamates as Inhibitors of Fatty Acid Amide Hydrolase: Biological Activity and in vitro Metabolic Stability

ChemMedChem ◽  
2016 ◽  
Vol 11 (4) ◽  
pp. 429-443 ◽  
Author(s):  
Tobias Terwege ◽  
Walburga Hanekamp ◽  
David Garzinsky ◽  
Simone König ◽  
Oliver Koch ◽  
...  
Keyword(s):  
Biological Activity ◽  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Metabolic Stability ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

scholarly journals Design, Synthesis, and In Vitro Evaluation of Carbamate Derivatives of 2-Benzoxazolyl- and 2-Benzothiazolyl-(3-hydroxyphenyl)-methanones as Novel Fatty Acid Amide Hydrolase Inhibitors

2007 ◽  
Vol 50 (17) ◽  
pp. 4236-4242 ◽  
Author(s):  
Mikko J. Myllymäki ◽  
Susanna M. Saario ◽  
Antti O. Kataja ◽  
Joel A. Castillo-Melendez ◽  
Tapio Nevalainen ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Design Synthesis ◽  
In Vitro Evaluation ◽  
Amide Hydrolase ◽  
Derivatives Of ◽  
Fatty Acid Amide

scholarly journals Design, Synthesis, and In Vitro Evaluation of Carbamate Derivatives of 2-Benzoxazolyl- and 2-Benzothiazolyl-(3-hydroxyphenyl)-methanones as Novel Fatty Acid Amide Hydrolase Inhibitors.

2007 ◽  
Vol 50 (23) ◽  
pp. 5868-5868
Author(s):  
Mikko J. Myllymäki ◽  
Susanna M. Saario ◽  
Antti O. Kataja ◽  
Joel A. Castillo-Melendez ◽  
Tapio Nevalainen ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Design Synthesis ◽  
In Vitro Evaluation ◽  
Amide Hydrolase ◽  
Derivatives Of ◽  
Fatty Acid Amide

scholarly journals In Silico and In Vitro Analysis of Major Cannabis-Derived Compounds as Fatty Acid Amide Hydrolase Inhibitors

Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 48
Author(s):  
Emanuele Criscuolo ◽  
Maria Laura De Sciscio ◽  
Filomena Fezza ◽  
Mauro Maccarrone
Keyword(s):  
Fatty Acid ◽  
In Silico ◽  
Therapeutic Potential ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Integrated Approach ◽  
In Vitro Assays ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

Accumulated evidence suggests that enhancing the endocannabinoid (eCB) tone, in particular of anandamide (N-arachidonoylethanolamine, AEA), has therapeutic potential in many human diseases. Fatty acid amide hydrolase (FAAH) is a membrane-bound enzyme principally responsible for the degradation of AEA, and thus it represents a relevant target to increase signaling thereof. In recent years, different synthetic and natural compounds have been developed and tested on rat FAAH, but little is known of their effect on the human enzyme. Here, we sought to investigate six major cannabis-derived compounds to compare their action on rat and human FAAHs. To this aim, we combined an in silico analysis of their binding mode and affinity, with in vitro assays of their effect on enzyme activity. This integrated approach allowed to disclose differences in efficacy towards rat and human FAAHs, and to highlight the role of key residues involved in the inhibition of both enzymes. This study suggests that the therapeutic efficacy of compounds targeted towards FAAH should be always tested in vitro on both rat and human enzymes.

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