Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity

Marjolein Soethoudt, Uwe Grether, Jürgen Fingerle, +29

Nature Communications

Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474

Annelot C. M. van Esbroeck, Antonius P. A. Janssen, Armand B. Cognetta, +26

Science

Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition

Daisuke Ogasawara, Hui Deng, Andreu Viader, +17

Proceedings of the National Academy of Sciences

Diacylglycerol LipasesMolecular PhysiologySignal TransductionBiochemistryChemical Probes +13

The novel, orally available and peripherally restricted selective cannabinoid CB₂ receptor agonist LEI‐101 prevents cisplatin‐induced nephrotoxicity

Partha Mukhopadhyay, Marc P. Baggelaar, Katalin Erdélyi, +14

British Journal of Pharmacology

Development of an Activity‐Based Probe and In Silico Design Reveal Highly Selective Inhibitors for Diacylglycerol Lipase‐α in Brain

Marc P. Baggelaar, Freek J. Janssen, Annelot C. M. van Esbroeck, +12

Angewandte Chemie International Edition

Systems PharmacologyInhibitory ActivityProteinlipid InteractionDiacylglycerol Lipase‐αAbpp=activity-based Protein Profiling +13

Highly Selective, Reversible Inhibitor Identified by Comparative Chemoproteomics Modulates Diacylglycerol Lipase Activity in Neurons

Marc P. Baggelaar, Pascal Chameau, Vasudev Kantae, +17

Journal of the American Chemical Society

Proteinlipid InteractionDrug TargetDiacylglycerol LipaseLipid MovementReversible Inhibitor Identified +15

Mapping in vivo target interaction profiles of covalent inhibitors using chemical proteomics with label-free quantification

Eva J. van Rooden, Bogdan I. Florea, Hui Deng, +5

Nature Protocols

Molecular DockingCovalent InhibitorsDrug TargetBiochemistryChemical Proteomics +8

Chemical Proteomics Maps Brain Region Specific Activity of Endocannabinoid Hydrolases

Marc P. Baggelaar, Annelot C. M. van Esbroeck, Eva J. van Rooden, +5

ACS Chemical Biology

Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding

Hui Deng, Sander Kooijman, Adrianus M. C. H. van den Nieuwendijk, +11

Journal of Medicinal Chemistry

A palmitoyl transferase chemical–genetic system to map ZDHHC-specific S-acylation

Cory A. Ocasio, Marc P. Baggelaar, James Sipthorp, +13

Nature Biotechnology