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A Review on the Monoacylglycerol Lipase: At the Interface Between Fat and Endocannabinoid Signalling

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Abstract:

Together with anandamide, 2-arachidonoylglycerol (2-AG) constitutes one of the main representatives of a family of endogenous lipids known as endocannabinoids. These act by binding to CB1 and CB2 cannabinoid receptors, the molecular target of the psychoactive compound Δ9-THC, both in the periphery and in the central nervous system, where they behave as retrograde messengers to modulate synaptic transmission.

These last years, evidence has accumulated to demonstrate the lead role played by the monoacylglycerol lipase (MAGL) in the regulation of 2-arachidonoylglycerol (2-AG) levels. Considering the numerous physiological functions played by this endocannabinoid, MAGL is now considered a promising target for therapeutics, as inhibitors of this enzyme could reveal useful for the treatment of pain and inflammatory disorders, as well as in cancer research, among others.

Here we review the milestones that punctuated MAGL history, from its discovery to recent advances in the field of inhibitors development. An emphasis is given on the recent elucidation of the tridimensional structure of the enzyme, which could offer new opportunities for rational drug design.

Keywords: 2-arachidonoylglycerol; endocannabinoid system; inhibitor; monoacylglycerol lipase; monoglyceride lipase

Document Type: Research Article

DOI: http://dx.doi.org/10.2174/092986710791859414

Affiliations: Universite catholique de Louvain, Louvain Drug Research Institute, Cannabinoid and endocannabinoid research group, Pharmaceutical Chemistry Dpt, Avenue E. Mounier 73.40, 1200 Brussels, Belgium.

Publication date: August 1, 2010

More about this publication?
  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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