摘要：肿瘤的高生长率使得肿瘤细胞对氨基酸需求显著增高，LAT1（L-type amino acid transporter）是一类跨膜蛋白，能够特异性识别并运输大型中性氨基酸，通过持续为肿瘤细胞供给必需氨基酸来推动肿瘤的恶性增殖与进展。LAT1在多种恶性肿瘤中均呈现高表达特征，已成为极具临床转化前景的抗肿瘤治疗靶点。硼中子俘获疗法（Boron Neutron Capture Therapy, BNCT）是一种利用选择性硼积累和中子照射消灭癌细胞的先进放疗技术，LAT1正是提升BNCT靶向性与治疗效能的核心分子靶点。本综述阐述了多种LAT1靶向化合物的结构特征和生物活性，同时介绍了BNCT中LAT1靶向小分子的研究情况，并对LAT1在抗肿瘤药物靶向治疗方向进行讨论与展望。

Abstract：Tumor cell proliferation causes a considerable rise in the demand for amino acids. LAT1 (L-type amino acid transporter) is a transmembrane protein that identifies and transports large neutral amino acids, hence facilitating malignant tumor progression by continually supplying essential amino acids to cancer cells. LAT1 has been found to be overexpressed in a variety of malignant tumors. As a result, pharmaceutical interventions that target LAT1 function have emerged as a promising therapeutic strategy for cancer. BNCT (Boron Neutron Capture Therapy) is an advanced radiotherapy therapeutic approach that eliminates cancer cells by selectively accumulating boron and irradiating them with neutrons, with LAT1 serving as a core molecular target to improve BNCT specificity and therapeutic efficacy. This review elucidates the structural features and biological activities of multiple LAT1-targeting compounds, presents the current research state of LAT1-targeting small molecules in BNCT, and discusses the prospects for LAT1 in targeted antitumor drug therapy.