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首页> 外文期刊>Journal of Medicinal Chemistry >A Drosophila model to identify polyamine-drug conjugates that target the polyamine transporter in an intact epithelium
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A Drosophila model to identify polyamine-drug conjugates that target the polyamine transporter in an intact epithelium

机译：果蝇模型，以确定在完整的上皮细胞中靶向多胺转运蛋白的多胺-药物缀合物

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Polyamine transport is elevated in many tumor types, suggesting that toxic polyamine-drug conjugates could be targeted to cancer cells via the polyamine transporter (PAT). We have previously reported the use of Chinese hamster ovary (CHO) cells and its PAT-deficient mutant cell line, CHO-MG, to screen anthracene-polyamine conjugates for their PAT-selective targeting ability. We report here a novel Drosophila-based model for screening anthracene-polyamine conjugates in a developing and intact epithelium (Drosophila imaginal discs), wherein cell-cell adhesion properties are maintained. Data from the Drosophila assay are consistent with previous results in CHO cells, indicating that the Drosophila epithelium has a PAT with vertebrate-like characteristics. This assay will be of use to medicinal chemists interested in screening drugs that use PAT for cellular entry, and it offers the possibility of genetic dissection of the polyamine transport process, including identification of a Drosophila PAT.
机译：在许多肿瘤类型中，多胺转运增加，这表明有毒的多胺-药物偶联物可通过多胺转运蛋白（PAT）靶向癌细胞。我们以前曾报道过使用中国仓鼠卵巢（CHO）细胞及其PAT缺陷型突变细胞系CHO-MG，筛选蒽-多胺共轭物的PAT选择性靶向能力。我们在这里报告一种新颖的基于果蝇的模型，用于在发育中的和完整的上皮（果蝇假想盘）中筛选蒽-多胺共轭物，其中维持了细胞间粘附特性。果蝇试验的数据与CHO细胞中的先前结果一致，表明果蝇上皮具有具有脊椎动物样特征的PAT。该测定法对有兴趣筛选使用PAT进入细胞的药物的药用化学家有用，它提供了对多胺转运过程进行遗传解剖的可能性，包括果蝇PAT的鉴定。

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