The attachment of a benzyloxy group to the 5-position of the indole system of the LAT1 (SLC7A5) substrate amino acid l-Trp produced a moderately potent inhibitor of LAT1-mediated leucine transport in HT-29 cells, while no inhibition of LAT1 was observed for 4-, 6-, or 7-benzyloxy-l-Trp at concentrations below 100 μM. None of these benzyloxy-l-Trp residues was found to be a transport substrate. The extension of the benzyloxy group in 5-benzyloxy-l-Trp with aryl or heteroaryl moieties in most cases did not result in significant changes in LAT1 inhibitory activity.

中文翻译：

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l-色氨酸衍生物作为 l-型氨基酸转运蛋白 LAT1 (SLC7A5) 抑制剂的评价

苄氧基连接到 LAT1 (SLC7A5) 底物氨基酸l -Trp 的吲哚系统的 5 位上产生了一种中等强度的 LAT1 介导的 HT-29 细胞中亮氨酸转运的抑制剂，而 LAT1 没有抑制作用。在浓度低于 100 μM 时观察到 4-、6- 或 7-苄氧基-l -Trp。没有发现这些苄氧基-1- Trp残基是转运底物。在大多数情况下，用芳基或杂芳基部分扩展 5-苄氧基-l - Trp 中的苄氧基不会导致 LAT1 抑制活性的显着变化。