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Proteasome as a New Target for Bio‐Inspired Benzo[ k , l ]xanthene Lignans
Author(s) -
Capolupo Angela,
Tosco Alessandra,
Mozzicafreddo Matteo,
Tringali Corrado,
Cardullo Nunzio,
Monti Maria Chiara,
Casapullo Agostino
Publication year - 2017
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201701095
Subject(s) - xanthene , proteasome , chemistry , computational biology , in vitro , biochemistry , proteomics , biology , organic chemistry , gene
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.