ArticleNature communications2023
A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence.
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Article in Nature communications, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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28citing papers in PubMed
11.4field-weighted citation impact, top 1% of its field
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Who cites it
28 citing papers in PubMed, 47 citations in OpenAlex.
- Computational discovery and dynamic profiling of dual acetylcholinesterase and monoacylglycerol lipase inhibitors for Alzheimer's disease.Molecular diversity · 2026Article
- The Neurochemical Orchestra of the Runner's High: A Narrative Review of Neuromodulatory Mechanisms with a Focus on Endocannabinoids.The Neuroscientist : a review journal bringing neurobiology, neurology and psychiatry · 2026Review
- Article
- Endothelial cannabinoid CB1 receptor deficiency reduces shear stress-induced arterial inflammation and lipid uptake.Nature communications · 2026Article
- Recent Progress in the Development of Selective MAGL Modulators (2020-2026).Molecules (Basel, Switzerland) · 2026Review
- Tissue-specific roles of monoacylglycerol (MAG) in metabolic diseases.Immunometabolism (Cobham, Surrey) · 2026Review
- Development of Glycoconjugated MAGL Inhibitors with Glucose-Dependent Antiproliferative Activity.International journal of molecular sciences · 2026Article
- MAGL Inhibition Relieves Psoriasiform Inflammation and Pruritus Via Modulation of ALOX12-12-HETE Axis in Mice.Inflammation · 2026Article
- Multiple Roles of Cannabinoids in the Olfactory System.Brain sciences · 2026Review
- Cytosolic Versus Lysosomal Lipolysis in Adipose Tissue: Opposing Roles in Cardiometabolic Disease.Arteriosclerosis, thrombosis, and vascular biology · 2026Review
- FAAH and MAGL inhibition: Evolving approaches to treating substance use disorders.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2026Review
- Spatially Resolved Mapping of Monoacylglycerol Lipase Activity in the Brain.ACS chemical neuroscience · 2025Article
- Alcohol use disorder-associated pain: clinical and preclinical evidence.Alcohol (Fayetteville, N.Y.) · 2025Review
- Expediting hit-to-lead progression in drug discovery through reaction prediction and multi-dimensional optimization.Nature communications · 2025Article
- Lipolysis gone rogue: the HSL connection in feeding cancer.Cell biology and toxicology · 2025Review
- Circuit mechanisms governing endocannabinoid modulation of affective behaviour and stress adaptation.Nature reviews. Neuroscience · 2025Review
- Methods for Assessing MAGL Enzymatic Activity: An Extensive Review of Past and Emerging Approaches.International journal of molecular sciences · 2025Review
- Chronic intermittent ethanol produces nociception through endocannabinoid-independent mechanisms in mice.Neuropharmacology · 2025Article
- Article
- Endocannabinoid Tone and Oxylipins in Rheumatoid Arthritis and Osteoarthritis-A Novel Target for the Treatment of Pain and Inflammation?International journal of molecular sciences · 2025Article
Corrections and comments
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Authors and funding
29 authors at 3 institutions in 3 countries.
Ming Jiang *Department of Molecular Physiology, Leiden University & Oncode Institute, Leiden, Netherlands.
Mirjam C W Huizenga *Department of Molecular Physiology, Leiden University & Oncode Institute, Leiden, Netherlands.ORCID 0000-0001-8313-0019
Jonah L Wirt *Department of Psychological and Brain Sciences, Program in Neuroscience, Gill Center for Biomolecular Science, Indiana University, Bloomington, IN, USA.ORCID 0000-0001-5746-6678
Janos PalocziLaboratory of Cardiovascular Physiology and Tissue Injury, National Institute of Health/NIAAA, Rockville, MD, USA.ORCID 0000-0002-7691-4138
Avand AmediDepartment of Molecular Physiology, Leiden University & Oncode Institute, Leiden, Netherlands.
Richard J B H N van den BergDepartment of Bio-organic Synthesis, Leiden University, Leiden, Netherlands.
Joerg BenzRoche Innovation Center Basel, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
Ludovic CollinRoche Innovation Center Basel, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
Hui DengDepartment of Molecular Physiology, Leiden University & Oncode Institute, Leiden, Netherlands.
Xinyu DiMetabolomics and analytics center, Leiden University, Leiden, Netherlands.
Wouter F DrieverDepartment of Molecular Physiology, Leiden University & Oncode Institute, Leiden, Netherlands.ORCID 0000-0002-9250-0381
Bogdan I FloreaDepartment of Bio-organic Synthesis, Leiden University, Leiden, Netherlands.
Uwe GretherRoche Innovation Center Basel, F. Hoffmann-La Roche Ltd., Basel, Switzerland.ORCID 0000-0002-3164-9270
Antonius P A JanssenDepartment of Molecular Physiology, Leiden University & Oncode Institute, Leiden, Netherlands.ORCID 0000-0003-4203-261X
Thomas HankemeierMetabolomics and analytics center, Leiden University, Leiden, Netherlands.
Laura H HeitmanDivision of Drug Discovery and Safety, Leiden University & Oncode Institute, Leiden, Netherlands.ORCID 0000-0002-1381-8464
Tsang-Wai LamPivot Park Screening Centre, Oss, Netherlands.
Florian MohrDepartment of Molecular Physiology, Leiden University & Oncode Institute, Leiden, Netherlands.
Anto PavlovicRoche Innovation Center Basel, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
Iris RufRoche Innovation Center Basel, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
Helma van den HurkPivot Park Screening Centre, Oss, Netherlands.
Anna F StevensDepartment of Molecular Physiology, Leiden University & Oncode Institute, Leiden, Netherlands.ORCID 0000-0002-6688-4377
Daan van der VlietDepartment of Molecular Physiology, Leiden University & Oncode Institute, Leiden, Netherlands.ORCID 0000-0001-7317-9679
Tom van der WelDepartment of Molecular Physiology, Leiden University & Oncode Institute, Leiden, Netherlands.ORCID 0000-0002-6449-3233
Matthias B WittwerRoche Innovation Center Basel, F. Hoffmann-La Roche Ltd., Basel, Switzerland.ORCID 0000-0003-1359-4795
Constant A A van BoeckelDepartment of Molecular Physiology, Leiden University & Oncode Institute, Leiden, Netherlands.
Pal PacherLaboratory of Cardiovascular Physiology and Tissue Injury, National Institute of Health/NIAAA, Rockville, MD, USA.ORCID 0000-0001-7036-8108
Andrea G HohmannDepartment of Psychological and Brain Sciences, Program in Neuroscience, Gill Center for Biomolecular Science, Indiana University, Bloomington, IN, USA. hohmanna@indiana.edu.ORCID 0000-0003-0941-6435
Mario van der SteltDepartment of Molecular Physiology, Leiden University & Oncode Institute, Leiden, Netherlands. m.van.der.stelt@chem.leidenuniv.nl.ORCID 0000-0002-1029-5717
Leiden University · NLRoche (Switzerland) · CHIndiana University Bloomington · US
Funding
Project 3 - In vivo pharmacology of cannabinoid receptor probesP01DA009158 · NIDA · UNIVERSITY OF CONNECTICUT STORRS · PI Alexandros Makriyannis · 1994 to 2026
$26.0MINTEGRATIVE PREDOCTORAL TRAINING IN DRUG ABUSE RESEARCH AT INDIANA UNIVERSITYT32DA024628 · NIDA · TRUSTEES OF INDIANA UNIVERSITY · PI Andrea Grace Hohmann, Kenneth Mackie · 2008 to 2026
$3.1MCB2 Cannabinoid Mechanisms for Suppressing Opioid Tolerance and DependenceR01DA047858 · NIDA · TRUSTEES OF INDIANA UNIVERSITY · PI HOHMANN, ANDREA GRACE, MACKIE, KENNETH · 2019 to 2023
$2.6MA Novel Mechanism for Decreasing Opioid RewardR21DA042584 · NIDA · TRUSTEES OF INDIANA UNIVERSITY · PI HOHMANN, ANDREA GRACE, REBEC, GEORGE VINCENT · 2016 to 2017
$392kNIDA NIH HHS P01 DA009158NIDA NIH HHS R01 DA047858NIDA NIH HHS R21 DA042584NIDA NIH HHS T32 DA024628
Abstract
Monoacylglycerol lipase (MAGL) regulates endocannabinoid 2-arachidonoylglycerol (2-AG) and eicosanoid signalling. MAGL inhibition provides therapeutic opportunities but clinical potential is limited by central nervous system (CNS)-mediated side effects. Here, we report the discovery of LEI-515, a peripherally restricted, reversible MAGL inhibitor, using high throughput screening and a medicinal chemistry programme. LEI-515 increased 2-AG levels in peripheral organs, but not mouse brain. LEI-515 attenuated liver necrosis, oxidative stress and inflammation in a CCl
Indexed as
Monoacylglycerol LipasesMonoglyceridesAnalgesicsAnimalsEndocannabinoidsMiceMice, Inbred C57BLReceptor, Cannabinoid, CB1RimonabantAnalgesicsEndocannabinoidsMonoacylglycerol LipasesMonoglyceridesReceptor, Cannabinoid, CB1Rimonabant
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.