Poor selectivity, potential systemic toxicity and drug resistance are the main challenges associated with chemotherapeutic drugs. MCT1 and MCT4 and LAT1 play vital roles in tumour metabolism and growth by taking up nutrients and are thus potential targets for tumour therapy. An increasing number of studies have shown the feasibility of including these transporters as components of tumour-targeting therapy. Here, we summarize the recent progress in MCT1-, MCT4-and LAT1-based therapeutic strategies. First, protein structures, expression, relationships with cancer, and substrate characteristics are introduced. Then, different drug targeting and delivery strategies using these proteins have been reviewed, including designing protein inhibitors, prodrugs and nanoparticles. Finally, a dual targeted strategy is discussed because these proteins exert a synergistic effect on tumour proliferation. This article concentrates on tumour treatments targeting MCT1, MCT4 and LAT1 and delivery techniques for improving the antitumour effect. These innovative tactics represent current state-of-the-art developments in transporter-based antitumour drugs.

选择性差、潜在的全身毒性和耐药性是与化疗药物相关的主要挑战。MCT1和MCT4和LAT1通过吸收营养在肿瘤代谢和生长中发挥重要作用，因此是肿瘤治疗的潜在靶点。越来越多的研究表明，将这些转运蛋白作为肿瘤靶向治疗的组成部分是可行的。在这里，我们总结了基于 MCT1、MCT4 和 LAT1 的治疗策略的最新进展。首先，介绍了蛋白质结构、表达、与癌症的关系以及底物特征。然后，审查了使用这些蛋白质的不同药物靶向和递送策略，包括设计蛋白质抑制剂、前药和纳米颗粒。最后，讨论了双重靶向策略，因为这些蛋白质对肿瘤增殖发挥协同作用。本文重点介绍针对 MCT1、MCT4 和 LAT1 的肿瘤治疗以及提高抗肿瘤效果的递送技术。这些创新策略代表了基于转运蛋白的抗肿瘤药物的最新发展。