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  • Andrographolide derivatives target the KEAP1/NRF2 axis and possess potent anti-SARS-CoV-2 activity [Elektronski vir]
    Schulte, Bianca ...
    Naturally occurring compounds represent a vast pool of pharmacologically active entities. One of such compounds is andrographolide, which is endowed with many beneficial properties, including the ... activity against severe acute respiratory syndrome coronavirus type 2 (SARS-CoV-2). To initiate a drug repurposing or hit optimization campaign, it is imperative to unravel the primary mechanism(s) of the antiviral action of andrographolide. Here, we showed by means of a reporter gene assay that andrographolide exerts its anti-SARS-CoV-2 effects by inhibiting the interaction between Kelch-like ECH-associated protein 1 (KEAP1) and nuclear factor erythroid 2-related factor 2 (NRF2) causing NRF2 upregulation. Moreover, we demonstrated that subtle structural modifications of andrographolide could lead to derivatives with stronger on-target activities and improved physicochemical properties. Our results indicate that further optimization of this structural class is warranted to develop novel COVID-19 therapies.
    Vir: ChemMedChem. - ISSN 1860-7187 (Vol. 17, iss. 5, e202100732, 2022, str. 1-11)
    Vrsta gradiva - e-članek ; neleposlovje za odrasle
    Leto - 2022
    Jezik - angleški
    COBISS.SI-ID - 96813827

    Povezava(-e):

    https://chemistry-europe.onlinelibrary.wiley.com/doi/full/10.1002/cmdc.202100732
    DOI

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