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The small-molecule kinase inhibitor ceritinib, unlike imatinib, causes a significant disturbance of lipid membrane integrity: A combined experimental and MD study.
Author: BashawatMohammad, FischerMarkus, LuckMeike, LudwigKai, MüllerPeter, ScheidtHolger A, VogelAlexander, WerleMax
Original Abstract of the Article :
Ceritinib and imatinib are small-molecule protein kinase inhibitors which are applied as therapeutic agents against various diseases. The fundamentals of their clinical use, i.e. their pharmacokinetics as well as the mechanisms of the inhibition of the respective kinases, are relatively well studied...See full text at original site
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引用元:
https://doi.org/10.1016/j.chemphyslip.2023.105351
データ提供:米国国立医学図書館(NLM)
Ceritinib: A Powerful Drug with Potential Membrane Impact
Ceritinib and imatinib are small-molecule protein kinase inhibitors used to treat various diseases. While their mechanisms of action and pharmacokinetics are well-studied, their interactions with cell membranes remain relatively unexplored. This study investigates the membrane impact of ceritinib and imatinib, aiming to understand their potential for disrupting membrane integrity and triggering side effects.
Ceritinib: A More Significant Membrane Disruptor
The research revealed a significant difference in the membrane impact of ceritinib and imatinib. Ceritinib, unlike imatinib, demonstrated a strong affinity for lipid membranes, altering membrane order and affecting the permeability of polar solutes. The study's findings highlight the importance of considering the membrane impact of drugs, as it could contribute to potential toxic or cytotoxic side effects.
Understanding Drug-Membrane Interactions
This research underscores the need to carefully consider the membrane-disrupting potential of drugs, especially when designing new therapies. By understanding the intricate interactions between drugs and cell membranes, researchers can develop safer and more effective medications. It's like studying the delicate ecosystem of a desert, understanding how different elements interact to maintain balance and prevent disruptions.
Dr.Camel's Conclusion
This research is like uncovering hidden secrets in the vast desert of drug discovery, reminding us that even the most promising drugs can have unexpected interactions with cell membranes. Understanding these interactions is crucial for developing safer and more effective medications, ensuring that patients can navigate the journey of treatment with greater confidence.
Date :
- Date Completed 2023-11-20
- Date Revised 2023-11-20
Further Info :
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