对肝癌细胞具有选择性的乳清酸缺氧激活铂（IV）前药
Hypoxia Active Platinum(IV) Prodrugs of Orotic Acid Selective to Liver Cancer Cells.
作者信息
Maji Moumita, Bhattacharya Indira, Acharya Sourav, Chakraborty Manas Pratim, Gupta Arnab, Mukherjee Arindam
机构信息
Department of Chemical Sciences and Centre for Advanced Functional Materials, Indian Institute of Science Education and Research (IISER) Kolkata, Mohanpur 741246, West Bengal, India.
Department of Biological Sciences, Indian Institute of Science Education and Research (IISER) Kolkata, Mohanpur 741246, West Bengal, India.
出版信息
Inorg Chem. 2021 Apr 5;60(7):4342-4346. doi: 10.1021/acs.inorgchem.0c03803. Epub 2021 Mar 12.
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.
乳清酸的铂（IV）配合物选择性靶向肝癌细胞，在Hep G2细胞中显示出增强的活性和更高的摄取量。Hep G2细胞中有机阴离子转运体2（OAT2）相对较高的表达以及在OAT2抑制剂存在下毒性的降低表明其参与了配合物的摄取。与顺铂和奥沙利铂不同，它们对铜转运蛋白ATP7B的螯合具有抗性。
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