Cu-64-dithiocarbamate compounds for theragnostic applications: Preliminary in-vitro studies (Abstract in rivista)

Type
Label
  • Cu-64-dithiocarbamate compounds for theragnostic applications: Preliminary in-vitro studies (Abstract in rivista) (literal)
Anno
  • 2014-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1016/j.nucmedbio.2014.05.036 (literal)
Alternative label
  • Morellato, N.; Cicoria, G.; Gandin, V.; Salvarese, N.; Marzano, C.; Malizia, C.; Bolzati, C. (2014)
    Cu-64-dithiocarbamate compounds for theragnostic applications: Preliminary in-vitro studies
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Morellato, N.; Cicoria, G.; Gandin, V.; Salvarese, N.; Marzano, C.; Malizia, C.; Bolzati, C. (literal)
Pagina inizio
  • 634 (literal)
Pagina fine
  • 634 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 41 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali
  • 1 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo
  • 7 (literal)
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • University of Padua; PET Radiopharm S Orsola Malpighi; Consiglio Nazionale delle Ricerche (CNR) (literal)
Titolo
  • Cu-64-dithiocarbamate compounds for theragnostic applications: Preliminary in-vitro studies (literal)
Abstract
  • Cu-DEDC and Cu-PDTC (DEDC = diethyl-dithiocarbamate; PDTC = pyrrolidine-dithiocarbamate) are interesting complexes displaying potent proteasome-inhibitory and apoptosis-inducing activities. Using the corresponding 64Cu-labeled compound, as chemical probes, we investigated the accumulation of these 64Cu-complexes in human normal (HEK293) and cancer (MCF-7) cells under a range of conditions, working both in carrier-added (64Cu/Cu) and carrier-free conditions (64Cu). Selective accumulation of the 64Cu-complexes was found in tumour cells. For both 64Cu-complexes a linear increase of the %cell-uptake was observed and did not reach a plateau even in carrier-added conditions where high concentration of compounds (100 ?M) was used. No variation of the %cell-uptake was observed in temperature-dependent experiments suggesting for these compounds a passive uptake mechanism. The complexes were effluxed from the cells in the form of ionic Cu. These data clearly support the model in which the ligand acts as an ionophore for the metal ion. Actually, the intracellular metal accumulation is maximized when the cells were treated with the Cu-complexes; copper and ligand follow different uptake kinetics and reach different intracellular concentrations. Thus, copper overload originated by the complex dissociation was responsible for the cytotoxic effects. This research was supported by MIUR (PRIN 20097FJHPZ-004 and FIRB RBAP114AMK \"RINAME\"). (literal)
Prodotto di
Autore CNR

Incoming links:


Autore CNR di
Prodotto
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#rivistaDi
data.CNR.it