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首页> 外文期刊>Drug Target Insights >Targeting Gallium to Cancer Cells through the Folate Receptor
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Targeting Gallium to Cancer Cells through the Folate Receptor

机译：通过叶酸受体将镓靶向癌细胞

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The development of gallium(III) compounds as anti-cancer agents for both treatment and diagnosis is a rapidly developing field of research. Problems remain in exploring the full potential of gallium(III) as a safe and successful therapeutic agent or as an imaging agent. One of the major issues is that gallium(III) compounds have little tropism for cancer cells. We have combined the targeting properties of folic acid (FA) with long chain liquid polymer poly(ethylene glycol) (PEG) ‘spacers’. This FA-PEG unit has been coupled to the gallium coordination complex of 1,4,7,10-tetraazacyclo-dodecane-N,N′,N′′,N′′′-tetraacetic acid (DOTA) through amide linkages for delivery into target cells overexpressing the folate receptor (FR). In vitro cytotoxicity assays were conducted against a multi-drug resistant ovarian cell line (A2780/AD) that overexpresses the FR and contrasted against a FR free Chinese hamster ovary (CHO) cell line. Results are rationalized taking into account stability studies conducted in RPMI 1640 media and HEPES buffer at pH 7.4.
机译：镓（III）化合物作为治疗和诊断的抗癌药的开发是一个快速发展的研究领域。在探索镓（III）作为安全和成功的治疗剂或显像剂的全部潜力方面仍然存在问题。主要问题之一是镓（III）化合物对癌细胞几乎没有向性。我们将叶酸（FA）的靶向特性与长链液态聚合物聚乙二醇（PEG）“间隔物”结合在一起。该FA-PEG单元已通过酰胺键与1,4,7,10-四氮杂环十二烷-N，N'，N''，N'''-四乙酸（DOTA）的镓配位复合物偶联进入过度表达叶酸受体（FR）的靶细胞。针对多药耐药卵巢细胞系（A2780 / AD）进行了体外细胞毒性测定，该细胞系过度表达FR，并与不含FR的中国仓鼠卵巢（CHO）细胞系形成对比。考虑到在RPMI 1640培养基和pH 7.4的HEPES缓冲液中进行的稳定性研究，结果是合理的。

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