What question did this study set out to answer?

To determine whether delivering the anticancer drug doxorubicin specifically to mitochondria induces cellular toxicity and circumvents multidrug efflux pumps.

April 16, 2013ACS Chemical Biology

Targeted Delivery of Doxorubicin to Mitochondria

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Authors

GCGraham Ross ChamberlainUniversity of Toronto DTDavid V. TulumelloSanofi (Canada)SKShana O. KelleyBoston College

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In vitro study demonstrates that peptide-mediated mitochondrial targeting of doxorubicin retains cytotoxic efficacy in efflux pump-overexpressing cells, suggesting an approach to bypass drug...

Key Points

To determine whether delivering the anticancer drug doxorubicin specifically to mitochondria induces cellular toxicity and circumvents multidrug efflux pumps.
Conjugated doxorubicin, an inhibitor of DNA topoisomerase II, to a mitochondria-targeting peptide.
Evaluated cytotoxicity and drug retention in wild-type cell models and cell lines overexpressing a common multidrug efflux pump.
The mitochondrially targeted doxorubicin peptide conjugate induced significant cellular toxicity.
Unlike parent nuclear-localized doxorubicin, the targeted compound resisted cellular export in cell lines overexpressing efflux pumps, maintaining potent anticancer activity.

Cite This Study

Chamberlain et al. (2013) studied this question.

synapsesocial.com/papers/6a765dc3f6749a0058ebfee6 https://doi.org/10.1021/cb400095v

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Implication

In vitro study demonstrates that peptide-mediated mitochondrial targeting of doxorubicin retains cytotoxic efficacy in efflux pump-overexpressing cells, suggesting an approach to bypass drug...

Targeted Delivery of Doxorubicin to Mitochondria

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Implication

Key Points

Cite This Study

Targeted Delivery of Doxorubicin to Mitochondria

Discussion

Member takes

Implication

Key Points

Cite This Study

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