Mass spectrometry-based chemical proteomics is a powerful tool in the target discovery of small molecules. Here we present the application of this approach 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 and in vitro and in cell fluorescence assays gave insights on the molecular mechanism of interaction, highlighting the the attitude of these lignans to inhibit the proteasome.

Proteasome as a new target for bio-inspired benzo[k,l]xanthene lignans

CAPOLUPO, ANGELA;TOSCO, ALESSANDRA;MONTI, Maria Chiara;CASAPULLO, Agostino
2017-01-01

Abstract

Mass spectrometry-based chemical proteomics is a powerful tool in the target discovery of small molecules. Here we present the application of this approach 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 and in vitro and in cell fluorescence assays gave insights on the molecular mechanism of interaction, highlighting the the attitude of these lignans to inhibit the proteasome.
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11386/4683253
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? 3
  • Scopus 9
  • ???jsp.display-item.citation.isi??? 9
social impact