NDLI: The energy blocker inside the power house: mitochondria targeted delivery of 3-bromopyruvate

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Chemical Science Vol - 6 Issue - 2

Chemical Science Vol -5

Chemical Science Vol -4

Chemical Science Vol -3

Chemical Science Vol -2

Chemical Science Vol -1

The energy blocker inside the power house: mitochondria targeted delivery of 3-bromopyruvate

Content Provider	Royal Society of Chemistry (RSC)
Author	Dhar, Shanta Marrache, Sean
Copyright Year	2015
Abstract	A key hallmark of many aggressive cancers is accelerated glucose metabolism. The enzymes that catalyze the first step of glucose metabolism are hexokinases. Elevated levels of hexokinase 2 (HK2) are found in cancer cells, but only in a limited number of normal tissues. Metabolic reprogramming of cancer cells using the energy blocker 3-bromopyruvate (3-BP), which inhibits HK2, has the potential to provide tumor-specific anticancer agents. However, the unique structural and functional characteristics of mitochondria prohibit selective subcellular targeting of 3-BP to modulate the function of this organelle for therapeutic gain. A mitochondria-targeted gold nanoparticle (T-3-BP-AuNP), decorated with 3-BP and delocalized lipophilic triphenylphosphonium cations to target the mitochondrial membrane potential (Δψm), was developed for delivery of 3-BP to cancer cell mitochondria by taking advantage of the higher Δψm in cancer cells compared to normal cells. In vitro studies demonstrated an enhanced anticancer activity of T-3-BP-AuNPs compared to the non-targeted construct NT-3-BP-AuNP or free 3-BP. The anticancer activity of T-3-BP-AuNPs was further enhanced upon laser irradiation by exciting the surface plasmon resonance band of AuNP and thereby utilizing a combination of 3-BP chemotherapeutic and AuNP photothermal effects. The lower toxicity of T-3-BP-NPs in normal mesenchymal stem cells indicated that these NPs preferentially kill cancer cells. T-3-BP-AuNPs showed an enhanced ability to modulate cancer cell metabolism by inhibiting glycolysis as well as demolishing mitochondrial oxidative phosphorylation. Our findings demonstrate that concerted chemo-photothermal treatment of glycolytic cancer cells with a single NP capable of targeting mitochondria, mediating simultaneous release of a glycolytic inhibitor and photothermal ablation, may have promise as a new anticancer therapy.
Starting Page	1832
Ending Page	1845
Page Count	14
File Format	HTM / HTML PDF
ISSN	20416520
Volume Number	6
Issue Number	3
Journal	Chemical Science
DOI	10.1039/c4sc01963f
Language	English
Publisher	Royal Society of Chemistry
Access Restriction	Subscribed
Subject Keyword	Mesenchymal stem cell NP Nanoparticle Enzyme inhibitor Glucose Metabolism Reuptake inhibitor Surface plasmon Hexokinase Mitochondrion Photothermal therapy Neurotrophin-3 Oxidative phosphorylation Laser Organelle Glycolysis Surface plasmon resonance Membrane potential Bromopyruvic acid Lipophilicity Cancer
Content Type	Text
Resource Type	Article
Subject	Chemistry

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Inhibition of hexokinase-2 with targeted liposomal 3-bromopyruvate in an ovarian tumor spheroid model of aerobic glycolysis.

Inhibition of hexokinase-2 with targeted liposomal 3-bromopyruvate in an ovarian tumor spheroid model of aerobic glycolysis

3-Bromopyruvic acid regulates glucose metabolism by targeting the c-Myc/TXNIP axis and induces mitochondria-mediated apoptosis in TNBC cells.

Age-Related Changes in Bone-Marrow Mesenchymal Stem Cells

Enhancing oxidative phosphorylation over glycolysis for energy production in cultured mesenchymal stem cells.

Elevated hexokinase increases cardiac glycolysis in transgenic mice (2001)

The antitumor effect and hepatotoxicity of a hexokinase II inhibitor 3-bromopyruvate: in vivo investigation of intraarterial administration in a rabbit VX2 hepatoma model.

The energy blocker inside the power house: mitochondria targeted delivery of 3-bromopyruvate

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Inhibition of hexokinase-2 with targeted liposomal 3-bromopyruvate in an ovarian tumor spheroid model of aerobic glycolysis.

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The energy blocker inside the power house: mitochondria targeted delivery of 3-bromopyruvate