Potentiation of mitochondrial dysfunction in tumor cells by conjugates of metabolic modulator dichloroacetate with a Pt(IV) derivative of oxaliplatin
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- 作者：Juraj Zajaca ; b ; Hana Kostrhunovaa ; Vojtech Novohradskya ; Oldrich Vranaa ; Raji Raveendranc ; Dan Gibsonc ; Jana Kasparkovab ; Viktor Brabeca ; brabec@ibp.cz" class="auth_mail" title="E-mail the corresponding author
- 关键词：Platinum-dichloroacetate conjugates ; Mitochondrial dysfunction ; Glucose metabolism ; Autophagy ; 5-Fluorouracil ; Cancer therapy
- 刊名：Journal of Inorganic Biochemistry
- 出版年：2016
- 出版时间：March 2016
- 年：2016
- 卷：156
- 期：Complete
- 页码：89-97
- 全文大小：567 K
文摘
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Pt(IV) derivatives of oxaliplatin conjugated with dichloroacetate were synthesized.
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Conjugates display markedly enhanced activity in cisplatin resistant tumor cells.
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DCA released in cancer cells affects mitochondria and metabolism of glucose.
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Conjugates activate an autophagic response in cancer cells.
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Toxicity of the conjugates in cancer cells can be potentiated by 5-fluorouracil.
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