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.
Proteasome as a New Target for Bio-Inspired Benzo[k,l]xanthene Lignans / Capolupo, A.; Tosco, A.; Mozzicafreddo, M.; Tringali, C.; Cardullo, N.; Monti, M. C.; Casapullo, A.. - In: CHEMISTRY-A EUROPEAN JOURNAL. - ISSN 0947-6539. - 23:35(2017), pp. 8371-8374. [10.1002/chem.201701095]
Proteasome as a New Target for Bio-Inspired Benzo[k,l]xanthene Lignans
Mozzicafreddo M.;
2017-01-01
Abstract
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
