Artemisinin Derivative FO-ARS-123 as a Novel VEGFR2 Inhibitor Suppresses Angiogenesis, Cell Migration, and Invasion
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- Conference
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- Abstract
- Anti-angiogenesis targeting vascular endothelial growth factor receptor 2 (VEGFR2) has been considered an important strategy for cancer therapy. VEGFR2 inhibitors targeting tumor angiogenic pathways have been widely used in clinical cancer treatment. However, inherent or acquired resistance to anti-angiogenic drugs may occur and thus limit their clinical application. New VEGFR2 inhibitors are still highly demanded. This study aimed to investigate VEGFR2-targeted artemisinin (ARS)-type compounds for cancer treatment. Here, we reported the ARS derivative FO-ARS-123 as a novel VEGFR2 inhibitor, which displayed potent binding activity with VEGFR2 in silico by molecular docking (pKi, 0.40 ±0.31 nM) and in vitro by microscale thermophoresis (Kd, 1.325 ±0.055 μM). In addition, compound FO-ARS-123 displayed a strong inhibition on cell proliferation of a broad range of cancer cells as well as suppressed cell migration and invasion. Remarkably, FO-ARS-123 exerted profound anti-angiogenesis effects in the in vitro tube formation assay and in vivo CAM assay. These results suggest that FO-ARS-123 might be a novel and promising anti-angiogenesis agent for cancer treatment.
- Autoren
- xiaohua Lu
- Conference finish date
- 2023
- Conference place
- Antalya, Turkiye
- Name of conference
- PSE meeting 2023 | PSE Natural Drug Discovery, Current Approach and Future Perspectives
- Datum der Datenerfassung
- 2023
- Conference start date
- 2023
- Titel
- Artemisinin Derivative FO-ARS-123 as a Novel VEGFR2 Inhibitor Suppresses Angiogenesis, Cell Migration, and Invasion
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