Mass spectrometry-based chemical proteomics is apowerful tool in the target discovery of small molecules. Here wepresent the application of this approach to define the target profile ofbio-inspired synthetic benzo[k,l]xanthene lignans, endowed withinteresting biological properties. Proteasome has been identified asa new main interactor for this class of compounds. A combination ofmolecular docking and in vitro and in cell fluorescence assays gaveinsights on the molecular mechanism of interaction, highlighting thethe attitude of these lignans to inhibit the proteasome.
Proteasome as a New Target for Bio-Inspired Benzo[k,l]xanthene Lignans
TRINGALI, Corrado;CARDULLO, NUNZIO;
2017-01-01
Abstract
Mass spectrometry-based chemical proteomics is apowerful tool in the target discovery of small molecules. Here wepresent the application of this approach to define the target profile ofbio-inspired synthetic benzo[k,l]xanthene lignans, endowed withinteresting biological properties. Proteasome has been identified asa new main interactor for this class of compounds. A combination ofmolecular docking and in vitro and in cell fluorescence assays gaveinsights on the molecular mechanism of interaction, highlighting thethe attitude of these lignans to inhibit the proteasome.File in questo prodotto:
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