Abstract
Platinum(IV) complexes of orotic acid selectively target liver cancer cells displaying enhanced activity and higher uptake in Hep G2. The comparatively higher expression of Organic Anion Transporter 2 (OAT2) in Hep G2 and decrease in toxicity in the presence of OAT2 inhibitor suggest its involvement in the uptake of the complexes. They are resistant to sequestration by the copper transporter ATP7B, unlike cisplatin and oxaliplatin.
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Cell Hypoxia / drug effects*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Humans
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Liver Neoplasms / drug therapy*
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Liver Neoplasms / metabolism
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Liver Neoplasms / pathology
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Molecular Structure
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Organic Anion Transporters, Sodium-Independent / antagonists & inhibitors
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Organic Anion Transporters, Sodium-Independent / metabolism
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Organoplatinum Compounds / chemical synthesis
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Organoplatinum Compounds / chemistry
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Organoplatinum Compounds / pharmacology*
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Orotic Acid / chemistry
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Orotic Acid / pharmacology*
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Prodrugs / chemical synthesis
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Prodrugs / chemistry
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Prodrugs / pharmacology*
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Organic Anion Transporters, Sodium-Independent
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Organoplatinum Compounds
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Prodrugs
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SLC22A7 protein, human
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Orotic Acid