Abstract
We developed a dual-target theranostic F671, which could exhibit synergetic anticancer effects for inhibiting the activities of glutathione S-transferase and the accumulation of hypoxia inducible factor-1α. F671 undergoes self-immolative cleavage when exposed to GSTP1-1 in live cancer cells, facilitating the visualization of molecule release and distribution, as well as confirming the autophagy-induced apoptosis.
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / metabolism
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents / therapeutic use
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Apoptosis / drug effects
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Autophagy
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Carcinoma, Hepatocellular / diagnostic imaging
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Carcinoma, Hepatocellular / drug therapy
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Cell Line, Tumor
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Female
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Glutathione S-Transferase pi / antagonists & inhibitors*
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Humans
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Hypoxia-Inducible Factor 1, alpha Subunit / antagonists & inhibitors*
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Intracellular Membranes / drug effects
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Liver Neoplasms / diagnostic imaging
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Liver Neoplasms / drug therapy
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Lysosomes / drug effects
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Lysosomes / metabolism
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Mice, Inbred BALB C
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Neoplasm Transplantation
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Oxadiazoles / chemical synthesis
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Oxadiazoles / metabolism
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Oxadiazoles / pharmacology*
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Oxadiazoles / therapeutic use
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Prodrugs / chemical synthesis
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Prodrugs / pharmacology
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Prodrugs / therapeutic use
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Theranostic Nanomedicine
Substances
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Antineoplastic Agents
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HIF1A protein, human
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Hif1a protein, mouse
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Hypoxia-Inducible Factor 1, alpha Subunit
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Oxadiazoles
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Prodrugs
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GSTP1 protein, human
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Glutathione S-Transferase pi
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Gstp1 protein, mouse