Platinum (II) complex-nuclear localization sequence peptide hybrid for overcoming platinum resistance in cancer therapy.,ACS Biomaterials Science & Engineering

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Platinum (II) complex-nuclear localization sequence peptide hybrid for overcoming platinum resistance in cancer therapy.
ACS Biomaterials Science & Engineering ( IF 5.4 ) Pub Date : 2018-01-09 , DOI: 10.1021/acsbiomaterials.7b00921
Marek T Wlodarczyk _{1,

2} , Sylwia A Dragulska ₁ , Olga Camacho-Vanegas ₃ , Peter R Dottino ₄ , Andrzej A Jarzęcki ₁ , John A Martignetti _{3,

5} , Aneta J Mieszawska ₁

Affiliation

Platinum therapy represents 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.

中文翻译：

铂（II）复杂核定位序列肽杂合体，用于克服癌症治疗中的铂抗性。

铂金疗法代表了许多恶性肿瘤的治疗的第一线，但其高全身毒性限制了治疗剂量。在此，我们报告了具有叠氮和炔烃官能团的卡铂类复合物的合成以及铂（II）-核定位序列肽（Pt-NLS）杂化物的形成，以改善铂（II）配合物直接导入到细胞核。Pt-NLS杂种成功进入细胞及其细胞核，形成Pt诱导的核损伤。在相同浓度下，Pt-NLS的体外功效很高，优于天然卡铂。所使用的方法简单且经济高效，最重要的是可以轻松扩展以将Pt（II）负载到其他支持物上，从而为增强Pt（II）疗法的递送开辟了新的可能性。

更新日期：2018-01-09

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