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Updated: Oct 23, 2025
Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
Published on: July 30, 2020
Natural anthraquinone compound emodin as a novel inhibitor of aurora A kinase: A pilot study
Fen-Lan Wu1, Pei-Yi Chu2, Guan-Yu Chen2
1Department of Obstetrics and Gynecology, Suzhou BenQ Medical Center, The Affiliated BenQ Hospital of Nanjing Medical University, Suzhou, China.
Abstract:
Aurora kinase A (AURKA) carries out an essential role in proliferation and involves in cisplatin resistance in various cancer cells. Overexpression of AURKA is associated with the poor prognosis of cancer patients. Thus, AURKA has been considered as a target for cancer therapy. Developing AURKA inhibitors became an important issue in cancer therapy. A natural compound emodin mainly extracted from rhubarbs possesses anti-cancer properties. However, the effect of emodin on AURKA has never been investigated. In the present study, molecular docking analysis indicated that emodin interacts with AURKA protein active site. We also found nine emodin analogues from Key Organic database by using ChemBioFinder software. Among that, one analogue 8L-902 showed a similar anti-cancer effect as emodin. The bindings of emodin and 8L-902 on AURKA protein were confirmed by cellular thermal shift assay. Furthermore, emodin inhibited the AURKA kinase activity in vitro and enhanced the cisplatin-DNA adduct level in a resistant ovarian cancer cell line. It seems that emodin may have the potential to inhibit cancer cell growth and enhance cisplatin therapy in cancer with resistance. Collectively, our finding reveals a novel AURKA inhibitor, emodin, which may be vulnerable to ovarian cancer therapy in the future.
Insights
Emodin, a natural compound, shows potential as an Aurora kinase A (AURKA) inhibitor. This discovery could lead to new ovarian cancer therapies, especially for cisplatin-resistant cancers.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Aurora kinase A (AURKA) is crucial for cell proliferation and linked to cisplatin resistance in cancers.
- Overexpression of AURKA correlates with poor patient prognosis, making it a significant therapeutic target.
- Developing novel AURKA inhibitors is a key focus in cancer treatment strategies.
Purpose of the Study:
- To investigate the effect of the natural compound emodin on AURKA.
- To identify potential emodin analogues with anti-cancer properties.
- To explore emodin's efficacy in overcoming cisplatin resistance in ovarian cancer.
Main Methods:
- Molecular docking analysis to predict emodin's interaction with AURKA.
- Screening of emodin analogues using ChemBioFinder software.
- Cellular thermal shift assay (CETSA) to confirm protein-ligand binding.
- In vitro kinase assays and assessment of cisplatin-DNA adducts in resistant ovarian cancer cells.
Main Results:
- Molecular docking revealed emodin interacts with the AURKA active site.
- One emodin analogue, 8L-902, demonstrated comparable anti-cancer effects to emodin.
- Emodin binding to AURKA was confirmed via CETSA.
- Emodin inhibited AURKA kinase activity and increased cisplatin-DNA adducts in resistant ovarian cancer cells.
Conclusions:
- Emodin functions as a novel inhibitor of Aurora kinase A (AURKA).
- Emodin demonstrates potential in enhancing cisplatin efficacy against resistant ovarian cancers.
- This study highlights emodin as a promising candidate for future ovarian cancer therapeutic development.
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