title: A Cu(ii) complex targeting the translocator protein: in vitro and in vivo antitumor potential and mechanistic insights.
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.
authors.affiliation: School of Chemistry, National University of Ireland Galway, Ireland. andrea.erxleben@nuigalway.ie and Department of Chemistry, Maynooth University, Ireland.
authors.forename: D
authors.initials: D
authors.lastname: Montagner
authors.affiliation: Department of Chemistry, University of Liege, Belgium and Department of Chemical Science, University of Padua, Italy.
authors.forename: B
authors.initials: B
authors.lastname: Fresch
authors.affiliation: School of Chemistry, National University of Ireland Galway, Ireland. andrea.erxleben@nuigalway.ie.
authors.forename: K
authors.initials: K
authors.lastname: Browne
authors.affiliation: Department of Pharmaceutical and Pharmacological Science, University of Padua, Italy. valentina.gandin@unipd.it.
authors.forename: V
authors.initials: V
authors.lastname: Gandin
authors.affiliation: School of Chemistry, National University of Ireland Galway, Ireland. andrea.erxleben@nuigalway.ie.
authors.forename: A
authors.initials: A
authors.lastname: Erxleben
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D045744:Cell Line, Tumor; D003300:Copper / Q000737:chemistry*; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006801:Humans; D051379:Mice; D008958:Models, Molecular; D058990:Molecular Targeted Therapy; D009942:Organometallic Compounds / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D011487:Protein Conformation; D018079:Receptors, GABA / Q000737:chemistry / Q000378:metabolism*; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D018079:Receptors, GABA; C499229:TSPO protein, human; D003300:Copper