ArticleACS chemical biology2018
Development of a Multiplexed Activity-Based Protein Profiling Assay to Evaluate Activity of Endocannabinoid Hydrolase Inhibitors.
Article in ACS chemical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 43 citations in OpenAlex.
- Spatially Resolved Mapping of Monoacylglycerol Lipase Activity in the Brain.ACS chemical neuroscience · 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
- Microplate-Based Enzymatic Activity Assay Protocol Powered by Activity-Based Probes.Methods in molecular biology (Clifton, N.J.) · 2025Article
- Late-stage (radio)fluorination of alkyl phosphonates via electrophilic activation.Nature communications · 2024Article
- Computational and Experimental Drug Repurposing of FDA-Approved Compounds Targeting the Cannabinoid Receptor CB1.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Strategies for Competitive Activity-Based Protein Profiling in Small Molecule Inhibitor Discovery and Characterization.Israel journal of chemistry · 2023Article
- Inhibition of diacylglycerol lipase β modulates lipid and endocannabinoid levels in theFrontiers in endocrinology · 2023Article
- Chemical Probes to Control and Visualize Lipid Metabolism in the Brain.Accounts of chemical research · 2022Review
- A potent and selective inhibitor for the modulation of MAGL activity in the neurovasculature.PloS one · 2022Article
- Controlling Antibacterial Activity Exclusively with Visible Light: Introducing a Tetra-ortho-Chloro-Azobenzene Amino Acid.Chemistry (Weinheim an der Bergstrasse, Germany) · 2021Article
- A Superfamily-wide Activity Atlas of Serine Hydrolases inBiochemistry · 2021Article
- Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling.Analytical chemistry · 2021Article
- Structure-Activity Relationship Studies of α-Ketoamides as Inhibitors of the Phospholipase A and Acyltransferase Enzyme Family.Journal of medicinal chemistry · 2020Article
- Strategies for Tuning the Selectivity of Chemical Probes that Target Serine Hydrolases.Cell chemical biology · 2020Review
- Structure Dependent Determination of Organophosphate Targets in Mammalian Tissues Using Activity-Based Protein Profiling.Chemical research in toxicology · 2020Article
- Activity-based protein profiling of the human failing ischemic heart reveals alterations in hydrolase activities involving the endocannabinoid system.Pharmacological research · 2020Article
- Identification of α,β-Hydrolase Domain Containing Protein 6 as a Diacylglycerol Lipase in Neuro-2a Cells.Frontiers in molecular neuroscience · 2019Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Endocannabinoids, an important class of signaling lipids involved in health and disease, are predominantly synthesized and metabolized by enzymes of the serine hydrolase superfamily. Activity-based protein profiling (ABPP) using fluorescent probes, such as fluorophosphonate (FP)-TAMRA and β-lactone-based MB064, enables drug discovery activities for serine hydrolases. FP-TAMRA and MB064 have distinct, albeit partially overlapping, target profiles but cannot be used in conjunction due to overlapping excitation/emission spectra. We therefore synthesized a novel FP-probe with a green BODIPY as a fluorescent tag and studied its labeling profile in mouse proteomes. Surprisingly, we found that the reporter tag plays an important role in the binding potency and selectivity of the probe. A multiplexed ABPP assay was developed in which a probe cocktail of FP-BODIPY and MB064 visualized most endocannabinoid serine hydrolases in mouse brain proteomes in a single experiment. The multiplexed ABPP assay was employed to profile endocannabinoid hydrolase inhibitor activity and selectivity in the mouse brain.
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Registered trials
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.