ArticleMolecules (Basel, Switzerland)2019
Set-Up and Validation of a High Throughput Screening Method for Human Monoacylglycerol Lipase (MAGL) Based on a New Red Fluorescent Probe.
Article in Molecules (Basel, Switzerland), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 18 citations in OpenAlex.
- ABHD2 activity is not required for the non-genomic action of progesterone on human sperm.Human reproduction (Oxford, England) · 2026Article
- xCELLigence™ RTCA system in cancer biology: innovations in real-time functional profiling.Cytotechnology · 2026Review
- Methods for Assessing MAGL Enzymatic Activity: An Extensive Review of Past and Emerging Approaches.International journal of molecular sciences · 2025Review
- Discovery of MAGL Inhibition by Lophine Derivatives: An Unexpected Finding from Chemiluminescent Assay Development.Molecules (Basel, Switzerland) · 2025Article
- Highly Specific Miniaturized Fluorescent Monoacylglycerol Lipase Probes Enable Translational Research.Journal of the American Chemical Society · 2025Article
- A Highly Selective and Versatile Probe Platform for Visualization of Monoacylglycerol Lipase.Angewandte Chemie (International ed. in English) · 2025Article
- Fluorescence-Based Enzyme Activity Assay: Ascertaining the Activity and Inhibition of Endocannabinoid Hydrolytic Enzymes.International journal of molecular sciences · 2024Review
- 2-Arachidonoylglycerol Synthesis: Facile and Handy Enzymatic Method That Allows to Avoid Isomerization.Molecules (Basel, Switzerland) · 2022Article
- Small-Molecules as Chemiluminescent Probes to Detect Lipase Activity.International journal of molecular sciences · 2022Article
- A New Ultrasensitive Bioluminescence-Based Method for Assaying Monoacylglycerol Lipase.International journal of molecular sciences · 2021Article
- Symmetrically substituted dichlorophenes inhibitThe Journal of biological chemistry · 2020Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Monoacylglycerol lipase (MAGL) is a serine hydrolase that has a key regulatory role in controlling the levels of 2-arachidonoylglycerol (2-AG), the main signaling molecule in the endocannabinoid system. Identification of selective modulators of MAGL enables both to provide new tools for investigating pathophysiological roles of 2-AG, and to discover new lead compounds for drug design. The development of sensitive and reliable methods is crucial to evaluate this modulatory activity. In the current study, we report readily synthesized long-wavelength putative fluorogenic substrates with different acylic side chains to find a new probe for MAGL activity. 7-Hydroxyresorufinyl octanoate proved to be the best substrate thanks to the highest rate of hydrolysis and the best Km and Vmax values. In addition, in silico evaluation of substrates interaction with the active site of MAGL confirms octanoate resorufine derivative as the molecule of choice. The well-known MAGL inhibitors URB602 and methyl arachidonylfluorophosphonate (MAFP) were used for the assay validation. The assay was highly reproducible with an overall average Z' value of 0.86. The fast, sensitive and accurate method described in this study is suitable for low-cost high-throughput screening (HTS) of MAGL modulators and is a powerful new tool for studying MAGL activity.
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