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首页> 外文期刊>Analytical Biochemistry: An International Journal of Analytical and Preparative Methods >Development of a cell-based screening method for compounds that inhibit or are transported by large neutral amino acid transporter 1, a key transporter at the blood-brain barrier
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Development of a cell-based screening method for compounds that inhibit or are transported by large neutral amino acid transporter 1, a key transporter at the blood-brain barrier

机译：基于细胞的筛选方法的开发，用于抑制或被大型中性氨基酸转运蛋白1转运的化合物，该转运蛋白是血脑屏障的关键转运蛋白

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摘要

Large neutral amino acid transporter 1 (LAT1) transports neutral amino acids with aromatic or branched side chains as well as their derivatives or prodrugs. Because the transporter is highly expressed at the blood-brain barrier and in some tumor cells, it is a potential target to treat brain disease and cancer. Therefore, it is essential to develop a method to screen for LAT1 inhibitors or for therapeutic compounds that it can transport. In this study, one such method was developed that combines an in vitro cell-based assay with high-throughput ultra-performance liquid chromatography triple quadrupole mass spectrometry (UPLC-QQQ-MS). Using this method, candidate compounds could be tested for the ability to inhibit or to compete with uptake of gabapentin, an LAT1 substrate, in HT-29 cells, which abundantly express the transporter. Gabapentin uptake is measured by mass spectrometry, which requires as little as 6 min/sample and will enable analysis of large numbers of samples. We anticipate that the method will be useful to identify LAT1 inhibitors or substrates without the need for animals or radioactive labeling. (C) 2015 Elsevier Inc. All rights reserved.
机译：大型中性氨基酸转运蛋白1（LAT1）转运带有芳族或支链侧链的中性氨基酸，以及它们的衍生物或前药。由于转运蛋白在血脑屏障和某些肿瘤细胞中高表达，因此它是治疗脑部疾病和癌症的潜在靶标。因此，开发一种筛选LAT1抑制剂或可运输的治疗性化合物的方法至关重要。在这项研究中，开发了一种将体外基于细胞的检测与高通量超高效液相色谱三重四极杆质谱（UPLC-QQQ-MS）相结合的方法。使用这种方法，可以测试候选化合物在大量表达转运蛋白的HT-29细胞中抑制或竞争摄取加巴喷丁（一种LAT1底物）的能力。加巴喷丁的摄入量通过质谱法测量，每个样品仅需6分钟，并且可以分析大量样品。我们预期该方法将无需动物或放射性标记即可用于鉴定LAT1抑制剂或底物。 （C）2015 Elsevier Inc.保留所有权利。

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