Anti-Leukaemic Activity of Rilpivirine Is Mediated by Aurora A Kinase Inhibition
Abstract
:Simple Summary
Abstract
1. Introduction
2. Materials and Methods
2.1. Chemicals
2.2. Kinase Assay
2.3. Cell Culture
2.4. Cell Viability Assay
2.5. Colony Formation Assay
2.6. Cell Cycle Analysis
2.7. Apoptosis Analysis
2.8. Caspase-3/7 Activity Assay
2.9. Western Blotting
2.10. Animal Experiments
2.11. Pharmacokinetic Analysis
2.12. In Vivo Safety Profiles
2.13. In Vivo Anti-Cancer Efficacy Study
2.14. Statistical Analysis
3. Results
3.1. Rilpivirine Shows Significant Inhibitory Selectivity towards Aurora A Kinase
3.2. Rilpivirine Exhibits Anti-Proliferative Activities in Multiple Leukaemic Cell Lines
3.3. Rilpivirine Arrests Leukaemic Cells in the G2/M Phase of the Cell Cycle
3.4. Rilpivirine Induces Apoptosis and Caspase 3/7 Activation in Leukaemic Cells
3.5. Rilpivirine Inhibits Aurora A Autophosphorylation and Modulates the Cell Cycle and Apoptosis Regulatory Proteins
3.6. Rilpivirine Inhibits Leukaemic Tumour Growth In Vivo
3.7. Rilpivirine Enhanced the Anti-Proliferative Effect of Cytarabine in Leukaemic Cells
4. Discussion
5. Conclusions
Supplementary Materials
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
References
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Islam, S.; Rahaman, M.H.; Yu, M.; Noll, B.; Martin, J.H.; Wang, S.; Head, R. Anti-Leukaemic Activity of Rilpivirine Is Mediated by Aurora A Kinase Inhibition. Cancers 2023, 15, 1044. https://doi.org/10.3390/cancers15041044
Islam S, Rahaman MH, Yu M, Noll B, Martin JH, Wang S, Head R. Anti-Leukaemic Activity of Rilpivirine Is Mediated by Aurora A Kinase Inhibition. Cancers. 2023; 15(4):1044. https://doi.org/10.3390/cancers15041044
Chicago/Turabian StyleIslam, Saiful, Muhammed H. Rahaman, Mingfeng Yu, Benjamin Noll, Jennifer H. Martin, Shudong Wang, and Richard Head. 2023. "Anti-Leukaemic Activity of Rilpivirine Is Mediated by Aurora A Kinase Inhibition" Cancers 15, no. 4: 1044. https://doi.org/10.3390/cancers15041044