A Cu(ii) complex targeting the translocator protein: in vitro and in vivo antitumor potential and mechanistic insightsThe work of BF is supported by the Italian Ministero dell'Istruzione, Università e Ricerca - grant "Rita Levi Montalcini - 2013". The research of VG was supported by the University of Padova (Grants 60A04-0443, 60A04-3189 and 60A04-4015/15).Electronic supplementary information (ESI) available: Experimental and computational details, crystallographic data, additional cytotoxicity

A new Cu-based anticancer metallodrug which targets the translocator protein is reported. [CuBr 2 (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 experim...

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Bibliographic Details
Main Authors Montagner, D, Fresch, B, Browne, K, Gandin, V, Erxleben, A
Format Journal Article
LanguageEnglish
Published 20.12.2016
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Summary:A new Cu-based anticancer metallodrug which targets the translocator protein is reported. [CuBr 2 (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. A Cu complex targeting the translocator protein induces a 98% reduction of tumor mass in a murine tumor model.
Bibliography:The work of BF is supported by the Italian Ministero dell'Istruzione, Università e Ricerca - grant "Rita Levi Montalcini - 2013". The research of VG was supported by the University of Padova (Grants 60A04-0443, 60A04-3189 and 60A04-4015/15).
For ESI and crystallographic data in CIF or other electronic format see DOI
2
consumption data, TEM images, body weight changes of treated mice, ligand poses and TSPO-complex structures. CCDC
10.1039/c6cc08100b
Electronic supplementary information (ESI) available: Experimental and computational details, crystallographic data, additional cytotoxicity data, values of the scoring functions, RESP partial atomic charges, cellular ROS levels, mitochondrial membrane potential and O
1473112
ISSN:1359-7345
1364-548X
DOI:10.1039/c6cc08100b