Publication Details |
| Category | Text Publication |
| Reference Category | Journals |
| DOI | 10.1002/cmdc.202200088 |
| Title (Primary) | Front cover: Andrographolide derivatives target the KEAP1/NRF2 axis and possess potent anti-SARS-CoV-2 activity (ChemMedChem 5/2022) |
| Author | Schulte, B.; König, M.; Escher, B.I.
; Wittenburg, S.; Proj, M.; Wolf, V.; Lemke, C.; Schnakenburg, G.; Sosič, I.; Streeck, H.; Müller, C.E.; Gütschow, M.; Steinebach, C. |
| Source Titel | ChemMedChem |
| Year | 2022 |
| Department | ZELLTOX |
| Volume | 17 |
| Issue | 5 |
| Page From | e202200088 |
| Language | englisch |
| Topic | T9 Healthy Planet |
| Keywords | SARS-CoV-2; andrographolide; KEAP1/NRF2; natural products; medicinal chemistry |
| Abstract | 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. |
| Schulte, B., König, M., Escher, B.I., Wittenburg, S., Proj, M., Wolf, V., Lemke, C., Schnakenburg, G., Sosič, I., Streeck, H., Müller, C.E., Gütschow, M., Steinebach, C. (2022): Front cover: Andrographolide derivatives target the KEAP1/NRF2 axis and possess potent anti-SARS-CoV-2 activity (ChemMedChem 5/2022) ChemMedChem 17 (5), e202200088 10.1002/cmdc.202200088 |
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