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

Montagner, D.
; 
Fresch, B.
; 
Browne, K.
; 
Gandin, V.
; 
Erxleben, Andrea
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Publication Date
2016-12-01
Keywords
PERIPHERAL BENZODIAZEPINE-RECEPTOR, SELECTIVE LIGANDS, BINDING-AFFINITY, 18 KDA, TSPO, CANCER, SITES, MODEL
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Montagner, D., Fresch, B., Browne, K., Gandin, V., & Erxleben, A. (2017). A Cu(ii) complex targeting the translocator protein: in vitro and in vivo antitumor potential and mechanistic insights. Chemical Communications, 53(1), 134-137. doi: 10.1039/C6CC08100B
Abstract
A new Cu-based anticancer metallodrug which targets the translocator protein is reported. [CuBr2(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.
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Publisher
Royal Society of Chemistry
Publisher DOI
10.1039/c6cc08100b
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Attribution-NonCommercial-NoDerivs 3.0 Ireland
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School of Biological and Chemical Sciences (Scholarly Articles)