3 years ago

Proteasome as a New Target for Bio-Inspired Benzo[k,l]xanthene Lignans

Proteasome as a New Target for Bio-Inspired Benzo[k,l]xanthene Lignans
Angela Capolupo, Alessandra Tosco, Agostino Casapullo, Nunzio Cardullo, Maria Chiara Monti, Matteo Mozzicafreddo, Corrado Tringali
Mass spectrometry-based chemical proteomics is a powerful tool for the target discovery of small molecules. Here, the application of this approach is presented to define the target profile of bio-inspired synthetic benzo[k,l]xanthene lignans endowed with interesting biological properties. Proteasome has been identified as a new main interactor for this class of compounds. A combination of molecular docking with in vitro and in cell fluorescence assays gave insights on the molecular mechanism of the interaction, highlighting the tendency of these lignans to inhibit the proteasome. A bait for proteasome: Mass spectrometry-based chemical proteomics discloses the proteasome as main target of bio-inspired synthetic benzo[k,l]xanthene lignans. A combination of molecular docking with in vitro and in cell fluorescence assays gives insights on the molecular mechanism of the interaction

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/chem.201701095

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