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一种靶向转位蛋白的铜(II)配合物:体外和体内抗肿瘤潜力及机制见解

A Cu(ii) complex targeting the translocator protein: in vitro and in vivo antitumor potential and mechanistic insights.

作者信息

Montagner D, Fresch B, Browne K, Gandin V, Erxleben A

机构信息

School of Chemistry, National University of Ireland Galway, Ireland.

Department of Chemistry, University of Liege, Belgium and Department of Chemical Science, University of Padua, Italy.

出版信息

Chem Commun (Camb). 2016 Dec 20;53(1):134-137. doi: 10.1039/c6cc08100b.

Abstract

A new Cu-based anticancer metallodrug which targets the translocator protein is reported. [CuBr(TZ6)] elicits a remarkable in vitro cytotoxicity in sensitive and multidrug resistant cell lines and induces a 98% reduction of tumor mass in a murine tumor model. Target binding was studied by experimental and computational methods.

摘要

据报道,一种靶向转位蛋白的新型铜基抗癌金属药物。[CuBr(TZ6)]在敏感和多药耐药细胞系中表现出显著的体外细胞毒性,并在小鼠肿瘤模型中使肿瘤质量减少了98%。通过实验和计算方法研究了靶点结合情况。

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