The DOI matches its Crossref record; 9 of the 9 references it cites were found in a registry or an index.
Characterization of Monoacylglycerol Lipase Inhibition Reveals Differences in Central and Peripheral Endocannabinoid Metabolism
Open accessAbstract
SUMMARY Monoacylglycerol lipase (MAGL) is a principal degradative enzyme for the endocannabinoid 2-arachidonoylglycerol (2-AG). We recently reported a piperidine carbamate, JZL184, that inhibits MAGL with high potency and selectivity. Here, we describe a comprehensive mechanistic characterization of JZL184. We provide evidence that JZL184 irreversibly inhibits MAGL via carbamoylation the enzyme’s serine nucleophile. Functional proteomic analysis of mice treated with JZL184 revealed that this inhibitor maintains good selectivity for MAGL across a wide range of central and peripheral tissues. Interestingly, MAGL blockade produced marked, tissue-specific differences in monoglyceride metabolism, with brain showing the most dramatic elevations in 2-AG and peripheral tissues often showing greater changes in other monoglycerides. Collectively, these studies indicate that MAGL exerts tissue-dependent control over endocannabinoid and monoglyceride metabolism and designate JZL184 as a selective tool to characterize the functions of MAGL in vivo.
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Self-citationBrain monoglyceride lipase participating in endocannabinoid inactivation
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Monoacylglycerol lipase regulates a fatty acid network that promotes cancer pathogenesis
Nomura, D. K., Long, J. Z., Niessen, S., Hoover, H. S., Ng, S.-W., & Cravatt, B. F. (2010) · Cell · doi:10.1016/j.cell.2009.11.027 · Cited by 1,002
Self-citationEndocannabinoid Hydrolysis Generates Brain Prostaglandins That Promote Neuroinflammation
Nomura, D. K., Morrison, B. E., Blankman, J. L., Long, J. Z., Kinsey, S. G., Marcondes, M. C. G., Ward, A. M., Hahn, Y. K., Lichtman, A. H., Conti, B., et al. (2011) · Science · doi:10.1126/science.1209200 · Cited by 727
Self-citationLipolysis – A highly regulated multi-enzyme complex mediates the catabolism of cellular fat stores
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Chronic monoacylglycerol lipase blockade causes functional antagonism of the endocannabinoid system
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Self-citationThe Metabolic Serine Hydrolases and Their Functions in Mammalian Physiology and Disease
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Metadata
- Authors
- Long, J. Z., Nomura, D. K., & Cravatt, B. F.
- Venue
- Chemistry & Biology
- Publisher
- Elsevier BV
- Published
- 2009-07
- Volume
- 16
- Issue
- 7
- Pages
- 744-753
- ISSN
- 1074-5521 (ISSN-L)
- OpenAlex
- W2102260997
- Cited by
- 303
- References
- 9
- FWCI
- 15.37
- Type
- journal article
- Language
- en
- Open access
- bronze
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