Therapeutic potential of fatty acid amide hydrolase, monoacylglycerol lipase, and N-acylethanolamine acid amidase inhibitors

Tuo, Wei, Leleu-Chavain, Natascha, Spencer, John, Sansook, Supojjanee, Millet, Regis and Chavatte, Philippe (2017) Therapeutic potential of fatty acid amide hydrolase, monoacylglycerol lipase, and N-acylethanolamine acid amidase inhibitors. Journal of Medicinal Chemistry, 60 (1). pp. 4-46. ISSN 0022-2623

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Abstract

Fatty acid ethanolamides (FAEs) and endocannabinoids (ECs) have been shown to alleviate pain and inflammation, regulate motility and appetite, and produce anti-cancer, anxiolytic, and neuroprotective efficacies via cannabinoid receptor type 1 (CB1) or type 2 (CB2), or via peroxisome proliferator-activated receptor α (PPAR-α) stimulation. FAEs and ECs are synthesized by a series of endogenous enzymes, including N acylphosphatidylethanolamine-phospholipase D (NAPE-PLD), diacylglycerol lipase (DAGL), or phospholipase C (PLC), and their metabolism is mediated by several metabolic enzymes, including fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL), Nacylethanolamine acid amidase (NAAA), or cyclooxygenase-2 (COX-2). Over the last decades, increasing the concentration of FAEs and ECs through the inhibition of degrading enzymes has been considered to be a viable therapeutic approach to enhance their anti-nociceptive and anti-inflammatory effects, as well as protecting the nervous system.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Depositing User: John Spencer
Date Deposited: 14 Nov 2016 11:33
Last Modified: 30 Jul 2017 10:21
URI: http://sro.sussex.ac.uk/id/eprint/65416

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