4.6 Article

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

Journal

FRONTIERS IN CHEMISTRY
Volume 7, Issue -, Pages -

Publisher

FRONTIERS MEDIA SA
DOI: 10.3389/fchem.2019.00053

Keywords

chemical proteomics; bioactive neolignans; molecular docking; drug affinity responsive target stability; nuclear import

Funding

  1. MIUR ITALY PRIN 2015 Top-down and Bottom-up approach in the development of new bioactive chemical entities inspired on natural products scaffolds [2015MSCKCE_003]
  2. Universita degli Studi di Salerno [ORSA151559]

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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-beta 1 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-beta 1 translocation has been evaluated by in vitro assays.

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