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一种与 spermine 缀合的亲脂性 Pt(iv)前药,旨在消除卵巢癌中的癌症干细胞。

A spermine-conjugated lipophilic Pt(iv) prodrug designed to eliminate cancer stem cells in ovarian cancer.

机构信息

Department of Chemistry and Biochemistry, Kent State University, 224 Williams Hall, Kent, Ohio 44242, USA.

Beijing National Laboratory for Molecular Sciences, State Key Laboratory of Polymer Physics and Chemistry, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, P. R. China.

出版信息

Chem Commun (Camb). 2019 May 28;55(43):6106-6109. doi: 10.1039/c9cc02081k. Epub 2019 May 9.

Abstract

We developed a spermine-conjugated lipophilic Pt(iv) prodrug that is able to reduce the cancer stem cell population in ovarian cancer. The therapeutic effect is attributed to the hydrophobic tail and cationic spermine head group, the combination of which allows the Pt(iv) prodrug to localize in mitochondria and induce corresponding damage.

摘要

我们开发了一种具有聚赖氨酸缀合亲脂性的顺铂(IV)前药,能够减少卵巢癌细胞中的癌症干细胞群体。这种治疗效果归因于疏水性尾部和阳离子聚赖氨酸头基,它们的结合使顺铂(IV)前药能够定位于线粒体并诱导相应的损伤。

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