Platinum(II) Complex-Nuclear Localization Sequence Peptide Hybrid for Overcoming Platinum Resistance in Cancer Therapy

التفاصيل البيبلوغرافية
العنوان: Platinum(II) Complex-Nuclear Localization Sequence Peptide Hybrid for Overcoming Platinum Resistance in Cancer Therapy
المؤلفون: Wlodarczyk, Marek T., Dragulska, Sylwia A., Camacho-Vanegas, Olga, Dottino, Peter R., Jarzęcki, Andrzej A., Martignetti, John A., Mieszawska, Aneta J.
المصدر: ACS Biomaterials Science & Engineering; 20240101, Issue: Preprints
مستخلص: Platinum therapy represents the first line of treatment in many malignancies but its high systemic toxicity limits the therapeutic dosage. Herein, we report the synthesis of carboplatin-like complexes with azide and alkyne functional groups and the formation of a platinum (II)-nuclear localization sequence peptide (Pt-NLS) hybrid to improve the import of platinum (II) complexes directly into the cell’s nucleus. The Pt-NLS hybrid successfully enters cells and their nuclei, forming Pt-induced nuclear lesions. The in vitro efficacy of Pt-NLS is high, superior to native carboplatin at the same concentration. The methodology used is simple and cost-effective and most importantly can easily be extended to load the Pt (II) onto other supports, opening new possibilities for enhanced delivery of Pt (II) therapy.
قاعدة البيانات: Supplemental Index
الوصف
تدمد:23739878
DOI:10.1021/acsbiomaterials.7b00921