Zhang Ling, Sui Chengguang, Yang Wenhan, Luo Qiuhua
Department of Biotherapy, The First Affiliated Hospital of China Medical University, Shenyang 110001, China.
Department of Pharmacy, The First Affiliated Hospital of China Medical University, Shenyang 110001, China.
Asian J Pharm Sci. 2020 Mar;15(2):192-206. doi: 10.1016/j.ajps.2019.12.002. Epub 2020 Mar 5.
Amino acid transporters, which play a vital role in transporting amino acids for the biosynthesis of mammalian cells, are highly expressed in types of tumors. Increasing studies have shown the feasibility of amino acid transporters as a component of tumor-targeting therapy. In this review, we focus on tumor-related amino acid transporters and their potential use in tumor-targeting therapy. Firstly, the expression characteristics of amino acid transporters in cancer and their relationship with tumor growth are reviewed. Secondly, the recognition requirements are discussed, focusing on the "acid-base" properties, conformational isomerism and structural analogues. Finally, recent developments in amino acid transporter-targeting drug delivery strategies are highlighted, including prodrugs and nanocarriers, with special attention to the latest findings of molecular mechanisms and targeting efficiency of transporter-mediated endocytosis. We aim to offer related clues that might lead to valuable tumor-targeting strategies by the utilization of amino acid transporters.
氨基酸转运体在为哺乳动物细胞生物合成转运氨基酸过程中发挥着至关重要的作用，在多种肿瘤类型中高表达。越来越多的研究表明，氨基酸转运体作为肿瘤靶向治疗的一个组成部分具有可行性。在本综述中，我们聚焦于肿瘤相关氨基酸转运体及其在肿瘤靶向治疗中的潜在应用。首先，综述了氨基酸转运体在癌症中的表达特征及其与肿瘤生长的关系。其次，讨论了识别要求，重点关注“酸碱”性质、构象异构和结构类似物。最后，突出了氨基酸转运体靶向药物递送策略的最新进展，包括前药和纳米载体，特别关注转运体介导的内吞作用的分子机制和靶向效率的最新研究结果。我们旨在提供相关线索，以便通过利用氨基酸转运体来开发有价值的肿瘤靶向策略。
