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Front Cover: Andrographolide Derivatives Target the KEAP1/NRF2 Axis and Possess Potent Anti‐SARS‐CoV‐2 Activity (ChemMedChem 5/2022)
Author(s) -
Schulte Bianca,
König Maria,
Escher Beate I.,
Wittenburg Sophie,
Proj Matic,
Wolf Valentina,
Lemke Carina,
Schnakenburg Gregor,
Sosič Izidor,
Streeck Hendrik,
Müller Christa E.,
Gütschow Michael,
Steinebach Christian
Publication year - 2022
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202200088
Subject(s) - andrographolide , front cover , natural product , chemistry , vero cell , linker , stereochemistry , pubchem , combinatorial chemistry , biochemistry , cover (algebra) , in vitro , mechanical engineering , computer science , engineering , operating system
The Front Cover illustrates the natural product andrographolide, which modulates the abundance of the transcription factor NRF2, a substrate of the E3 ligase KEAP1. Previous studies identified that this drug possessed anti‐SARS‐CoV‐2 activity, but the mechanism of action remained unclear. The authors designed and synthesized novel andrographolide derivatives with a functional site to fine‐tune physicochemical properties and for linker attachment. The team assayed this new set of compounds in a cell‐based NRF2 reporter gene assay and determined their ability to decrease infectivity of virus‐treated Vero‐E6 cells. Data showed that NRF2 activation by compounds and inhibition of SARS‐CoV‐2 replication correlated well. The study opens new avenues to investigate natural products that target the KEAP1/NRF2 axis as anti‐SARS‐CoV‐2 agents. More information can be found in the Research Article by Christian Steinebach et al.
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