Potentiation of mitochondrial dysfunction in tumor cells by conjugates of metabolic modulator dichloroacetate with a Pt(IV) derivative of oxaliplatin

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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 Zajac^a ; ^b ; Hana Kostrhunova^a ; Vojtech Novohradsky^a ; Oldrich Vrana^a ; Raji Raveendran^c ; Dan Gibson^c ; Jana Kasparkova^b ; Viktor Brabec^a ; ^{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

class="label">•: Pt(IV) derivatives of oxaliplatin conjugated with dichloroacetate were synthesized.
class="label">•: Conjugates display markedly enhanced activity in cisplatin resistant tumor cells.
class="label">•: DCA released in cancer cells affects mitochondria and metabolism of glucose.
class="label">•: Conjugates activate an autophagic response in cancer cells.
class="label">•: Toxicity of the conjugates in cancer cells can be potentiated by 5-fluorouracil.

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