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Recent Progress in the Development of Selective MAGL Modulators (2020-2026)
Eva Landucci1,2, Chiara Lonzi1, Tommaso Bonomo1
1Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy.
Molecules (Basel, Switzerland)
|July 15, 2026
Summary
Selective modulators of Monoacylglycerol lipase (MAGL) are crucial for targeting inflammation, pain, and neurodegeneration. Recent advances have expanded the chemical space of MAGL inhibitors and alternative strategies for therapeutic development.
Area of Science:
- Biochemistry
- Pharmacology
- Medicinal Chemistry
Background:
- Monoacylglycerol lipase (MAGL) is a key enzyme linking the endocannabinoid system and lipid metabolism.
- MAGL regulates lipid mediators involved in inflammation, pain, neurodegeneration, and cancer.
- Its therapeutic relevance makes MAGL an attractive target for drug development.
Purpose of the Study:
- To provide a comprehensive overview of selective MAGL modulators reported from 2020 to the present.
- To highlight structural diversity and emerging strategies in MAGL modulation.
- To guide the rational design of next-generation MAGL-targeting agents.
Main Methods:
- Literature review of selective MAGL modulators (excluding patent literature and MAGL probes).
- Analysis of classical enzyme inhibitors and alternative strategies like targeted protein degradation.
- Assessment of MAGL activity using innovative computational and biochemical methods.
Main Results:
- Significant expansion of the chemical space for MAGL modulators.
- Identification of diverse structural classes and modulation strategies.
- Emergence of targeted protein degradation as a novel approach.
Conclusions:
- Selective MAGL modulators offer promising therapeutic potential for various diseases.
- Continued research in medicinal chemistry and computational approaches is vital.
- Rational design principles are essential for developing effective MAGL-targeting agents.
