Self-assembling nanoparticles encapsulating zoledronic acid revert multidrug resistance in cancer cells
The overexpression of ATP binding cassette (ABC) transporters makes tumor cells simultaneously resistant to several cytotoxic drugs. Impairing the energy metabolism of multidrug resistant (MDR) cells is a promising chemosensitizing strategy, but many metabolic modifiers are too toxic in vivo. We pre...
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2015
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Online Access: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4741618/ |
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pubmed-47416182016-03-03 Self-assembling nanoparticles encapsulating zoledronic acid revert multidrug resistance in cancer cells Kopecka, Joanna Porto, Stefania Lusa, Sara Gazzano, Elena Salzano, Giuseppina Giordano, Antonio Desiderio, Vincenzo Ghigo, Dario Caraglia, Michele De Rosa, Giuseppe Riganti, Chiara Research Paper The overexpression of ATP binding cassette (ABC) transporters makes tumor cells simultaneously resistant to several cytotoxic drugs. Impairing the energy metabolism of multidrug resistant (MDR) cells is a promising chemosensitizing strategy, but many metabolic modifiers are too toxic in vivo. We previously observed that the aminobisphosphonate zoledronic acid inhibits the activity of hypoxia inducible factor-1α (HIF-1α), a master regulator of cancer cell metabolism. Free zoledronic acid, however, reaches low intratumor concentration. We synthesized nanoparticle formulations of the aminobisphosphonate that allow a higher intratumor delivery of the drug. We investigated whether they are effective metabolic modifiers and chemosensitizing agents against human MDR cancer cells in vitro and in vivo. Impact Journals LLC 2015-09-09 /pmc/articles/PMC4741618/ /pubmed/26372812 Text en Copyright: © 2015 Kopecka et al. http://creativecommons.org/licenses/by/2.5/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. |
repository_type |
Open Access Journal |
institution_category |
Foreign Institution |
institution |
US National Center for Biotechnology Information |
building |
NCBI PubMed |
collection |
Online Access |
language |
English |
format |
Online |
author |
Kopecka, Joanna Porto, Stefania Lusa, Sara Gazzano, Elena Salzano, Giuseppina Giordano, Antonio Desiderio, Vincenzo Ghigo, Dario Caraglia, Michele De Rosa, Giuseppe Riganti, Chiara |
spellingShingle |
Kopecka, Joanna Porto, Stefania Lusa, Sara Gazzano, Elena Salzano, Giuseppina Giordano, Antonio Desiderio, Vincenzo Ghigo, Dario Caraglia, Michele De Rosa, Giuseppe Riganti, Chiara Self-assembling nanoparticles encapsulating zoledronic acid revert multidrug resistance in cancer cells |
author_facet |
Kopecka, Joanna Porto, Stefania Lusa, Sara Gazzano, Elena Salzano, Giuseppina Giordano, Antonio Desiderio, Vincenzo Ghigo, Dario Caraglia, Michele De Rosa, Giuseppe Riganti, Chiara |
author_sort |
Kopecka, Joanna |
title |
Self-assembling nanoparticles encapsulating zoledronic acid revert multidrug resistance in cancer cells |
title_short |
Self-assembling nanoparticles encapsulating zoledronic acid revert multidrug resistance in cancer cells |
title_full |
Self-assembling nanoparticles encapsulating zoledronic acid revert multidrug resistance in cancer cells |
title_fullStr |
Self-assembling nanoparticles encapsulating zoledronic acid revert multidrug resistance in cancer cells |
title_full_unstemmed |
Self-assembling nanoparticles encapsulating zoledronic acid revert multidrug resistance in cancer cells |
title_sort |
self-assembling nanoparticles encapsulating zoledronic acid revert multidrug resistance in cancer cells |
description |
The overexpression of ATP binding cassette (ABC) transporters makes tumor cells simultaneously resistant to several cytotoxic drugs. Impairing the energy metabolism of multidrug resistant (MDR) cells is a promising chemosensitizing strategy, but many metabolic modifiers are too toxic in vivo. We previously observed that the aminobisphosphonate zoledronic acid inhibits the activity of hypoxia inducible factor-1α (HIF-1α), a master regulator of cancer cell metabolism. Free zoledronic acid, however, reaches low intratumor concentration. We synthesized nanoparticle formulations of the aminobisphosphonate that allow a higher intratumor delivery of the drug. We investigated whether they are effective metabolic modifiers and chemosensitizing agents against human MDR cancer cells in vitro and in vivo. |
publisher |
Impact Journals LLC |
publishDate |
2015 |
url |
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4741618/ |
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1613533825425473536 |