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Fatty acid amide hydrolase: a potential target for next generation therapeutics.
Curr Pharm Des 2006; 12(6):759-72CP

Abstract

Endocannabinoids are amides, esters and ethers of long chain polyunsaturated fatty acids, which act as new lipid mediators. Anandamide (N-arachidonoylethanolamine; AEA) and 2-arachidonoylglycerol are the main endogenous agonists of cannabinoid receptors, able to mimic several pharmacological effects of Delta(9)-tetrahydrocannabinol, the active principle of Cannabis sativa preparations like hashish and marijuana. The activity of AEA at its receptors is limited by cellular uptake through a specific membrane transporter, followed by intracellular degradation by a fatty acid amide hydrolase (FAAH). Growing evidence demonstrates that FAAH is the critical regulator of the endogenous levels of AEA, suggesting that it may serve as an attractive therapeutic target for the treatment of human disorders. In particular, FAAH inhibitors may be next generation therapeutic drugs of potential value for the treatment of pathologies in the central nervous system and in the periphery. Here, the potential applications of these inhibitors for human disease will be reviewed, with an emphasis on the properties of hydro(pero)xy-anandamides. In fact, these oxygenated derivatives of AEA are the most powerful inhibitors of FAAH of natural origin as yet discovered. In addition, new insights into the promoter region of FAAH gene will be presented, and the therapeutic potential of mimetics of transcription factors of this gene in the management of human infertility will be discussed.

Authors+Show Affiliations

Department of Biomedical Sciences, University of Teramo, Italy. mmaccarrone@unite.it

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

16472164

Citation

Maccarrone, Mauro. "Fatty Acid Amide Hydrolase: a Potential Target for Next Generation Therapeutics." Current Pharmaceutical Design, vol. 12, no. 6, 2006, pp. 759-72.
Maccarrone M. Fatty acid amide hydrolase: a potential target for next generation therapeutics. Curr Pharm Des. 2006;12(6):759-72.
Maccarrone, M. (2006). Fatty acid amide hydrolase: a potential target for next generation therapeutics. Current Pharmaceutical Design, 12(6), pp. 759-72.
Maccarrone M. Fatty Acid Amide Hydrolase: a Potential Target for Next Generation Therapeutics. Curr Pharm Des. 2006;12(6):759-72. PubMed PMID: 16472164.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Fatty acid amide hydrolase: a potential target for next generation therapeutics. A1 - Maccarrone,Mauro, PY - 2006/2/14/pubmed PY - 2006/4/1/medline PY - 2006/2/14/entrez SP - 759 EP - 72 JF - Current pharmaceutical design JO - Curr. Pharm. Des. VL - 12 IS - 6 N2 - Endocannabinoids are amides, esters and ethers of long chain polyunsaturated fatty acids, which act as new lipid mediators. Anandamide (N-arachidonoylethanolamine; AEA) and 2-arachidonoylglycerol are the main endogenous agonists of cannabinoid receptors, able to mimic several pharmacological effects of Delta(9)-tetrahydrocannabinol, the active principle of Cannabis sativa preparations like hashish and marijuana. The activity of AEA at its receptors is limited by cellular uptake through a specific membrane transporter, followed by intracellular degradation by a fatty acid amide hydrolase (FAAH). Growing evidence demonstrates that FAAH is the critical regulator of the endogenous levels of AEA, suggesting that it may serve as an attractive therapeutic target for the treatment of human disorders. In particular, FAAH inhibitors may be next generation therapeutic drugs of potential value for the treatment of pathologies in the central nervous system and in the periphery. Here, the potential applications of these inhibitors for human disease will be reviewed, with an emphasis on the properties of hydro(pero)xy-anandamides. In fact, these oxygenated derivatives of AEA are the most powerful inhibitors of FAAH of natural origin as yet discovered. In addition, new insights into the promoter region of FAAH gene will be presented, and the therapeutic potential of mimetics of transcription factors of this gene in the management of human infertility will be discussed. SN - 1381-6128 UR - https://www.unboundmedicine.com/medline/citation/16472164/Fatty_acid_amide_hydrolase:_a_potential_target_for_next_generation_therapeutics_ L2 - http://www.eurekaselect.com/55977/article DB - PRIME DP - Unbound Medicine ER -