Reversible Monoacylglycerol Lipase Inhibitors: Discovery of a New Class of Benzylpiperidine Derivatives
Giulia Bononi, Miriana Di Stefano, Giulio Poli, Gabriella Ortore, Philip Meier, Francesca Masetto, Isabella Caligiuri, Flavio Rizzolio, Marco Macchia, Andrea Chicca, Amir Avan, Elisa Giovannetti, Chiara Vagaggini, Annalaura Brai, Elena Dreassi, Massimo Valoti, Filippo Minutolo, Carlotta Granchi, Jürg Gertsch, Tiziano Tuccinardi
Abstract
showed antiproliferative activity and apoptosis induction, as well as the ability to reduce cell migration in primary pancreatic cancer cultures, and displayed a synergistic interaction with the chemotherapeutic drug gemcitabine. These results suggest that the class of benzylpiperidine-based MAGL inhibitors have potential as a new class of therapeutic agents and MAGL could play a role in pancreatic cancer.
Topics & Concepts
Monoacylglycerol lipaseChemistryPancreatic cancerEnzymePharmacologyPancreatic lipaseCancerLipaseBiochemistryEndocannabinoid systemBiologyMedicineReceptorInternal medicineCannabis and Cannabinoid ResearchPharmacological Receptor Mechanisms and EffectsPancreatic function and diabetes