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标题:The hydroxyl epimer of doxorubicin controls the rate of formation of cytotoxic anthracycline-DNA adducts.
时间:2020-02-15 11:23:35
DOI:10.1007/s00280-012-2049-x
PMID:23263186
作者:Robert A. Forrest; Lonnie P. Swift; Benny J. Evison…
关键词:RESISTANT TUMOR-CELLS;BUTYRIC-ACID;FORMALDEHYDE;ADRIAMYCIN;ACTIVATION;APOPTOSIS
出版源: 《Cancer Chemotherapy & Pharmacology》 ,71 (3) :809-816
摘要:Epirubicin was developed as a semi-synthetic anthracycline derivative to circumvent the cardiotoxic limitations associated with the use of doxorubicin in the clinic. Anthracycline compounds have been demonstrated to form covalent drug-DNA adducts utilising endogenous and exogenous sources of formaldehyde; however, previous investigations of the formation of epirubicin-DNA adducts provide conflicting evidence for adduct formation. This work provides evidence that epirubicin acts to form drug-DNA adducts at physiologically relevant concentrations and demonstrates that the rate of formation of epirubicin-DNA adducts is slower than that observed for other anthracycline compounds, explaining why they are only detectable under defined experimental conditions. Formation of covalent epirubicin-DNA adducts improves the apoptotic profile of epirubicin and provides opportunities to overcome drug resistance and cardiotoxic limitations.
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目录:
  • The hydroxyl epimer of doxorubicin controls the rate of formation of cytotoxic anthracycline-DNA adducts
    • Abstract
    • Introduction
    • Materials and methods
      • Cell lines
      • Compounds
      • Western blotting
      • Propidium iodide (PI) uptake assay
      • Tetramethylrhodamine methyl ester (TMRM) uptake assay
      • In vitro crosslinking assay: drug--DNA adduct formation
      • In vitro crosslinking assay: drug--DNA adduct stability
      • In vitro transcription assay
    • Results and discussion
    • Conclusion
    • Acknowledgments
    • References

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