Glutamine transporters are integral to the metabolism of glutamine in both healthy tissues and cancerous cells, playing a pivotal role in maintaining amino acid balance, synthesizing biomolecules, and regulating redox equilibrium. Their critical functions in cellular metabolism make them promising targets for oncological therapies. Recent years have witnessed substantial progress in the field of glutamine transporters, marked by breakthroughs in understanding of their protein structures and the discovery of novel inhibitors, prodrugs, and radiotracers. This review provides a comprehensive update on the latest advancements in modulators targeting the glutamine transporter, with special attention given to LAT1 and ASCT2. It also discusses innovative approaches in drug design aimed at these transporters.

谷氨酰胺转运蛋白是健康组织和癌细胞中谷氨酰胺代谢不可或缺的一部分，在维持氨基酸平衡、合成生物分子和调节氧化还原平衡方面发挥着关键作用。它们在细胞代谢中的关键功能使它们成为肿瘤治疗的有希望的靶标。近年来，谷氨酰胺转运蛋白领域取得了实质性进展，其标志是对其蛋白质结构的理解取得了突破，并发现了新型抑制剂、前药和放射性示踪剂。本综述全面更新了针对谷氨酰胺转运蛋白的调节剂的最新进展，特别关注 LAT1 和 ASCT2。它还讨论了针对这些转运蛋白的药物设计创新方法。