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RESEARCH PRODUCT

Chemical Proteomics-Guided Identification of a Novel Biological Target of the Bioactive Neolignan Magnolol

Roberta EspositoChiara CassianoCorrado TringaliMaria Chiara MontiRaffaele RiccioAgostino CasapulloMatteo MozzicafreddoAlessandra Tosco

subject

bioactive neolignans02 engineering and technologyComputational biology010402 general chemistryProteomics01 natural scienceslcsh:Chemistrychemistry.chemical_compoundchemical proteomicsdrug affinity responsive target stabilityOriginal Researchbioactive neolignans; chemical proteomics; drug affinity responsive target stability; molecular docking; nuclear importbiologyChemistryDrug discoveryIn vitro toxicologyGeneral Chemistrymolecular docking021001 nanoscience & nanotechnologynuclear importMagnololBioactive compound0104 chemical sciencesChemistrylcsh:QD1-999Biological targetChaperone (protein)Direct bindingbiology.protein0210 nano-technology

description

Understanding the recognition process between bioactive natural products and their specific cellular receptors is of key importance in the drug discovery process. In this outline, some potential targets of Magnolol, a natural bioactive compound, have been identified by proteomic approaches. Among them, Importin-β1 has been considered as the most relevant one. A direct binding between Magnolol and this nuclear chaperone has been confirmed by DARTS and molecular docking, while its influence on Importin-β1 translocation has been evaluated by in vitro assays.

10.3389/fchem.2019.00053https://www.frontiersin.org/article/10.3389/fchem.2019.00053/full