Amino acid transporters: Emerging roles in drug delivery for tumor-targeting therapy
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Updated: Dec 22, 2025

Author Spotlight: Exploring the Role of Ion Channels in Cancer: Characterization and Potential Treatment Approaches
Published on: June 16, 2023
Ling Zhang1, Chengguang Sui1, Wenhan Yang2,3
1Department of Biotherapy, The First Affiliated Hospital of China Medical University, Shenyang 110001, China.
Abstract:
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.
Insights
Amino acid transporters are highly expressed in tumors, offering a promising target for cancer therapy. This review explores their role in tumor growth and novel drug delivery strategies for targeted treatment.
Area of Science:
- Biochemistry
- Oncology
- Pharmacology
Background:
- Amino acid transporters are crucial for mammalian cell biosynthesis and are often overexpressed in various tumor types.
- Their elevated expression in cancer cells presents a viable target for developing novel tumor-targeting therapies.
Purpose of the Study:
- To review tumor-related amino acid transporters and their potential applications in cancer therapy.
- To discuss the recognition requirements of these transporters, including acid-base properties, isomerism, and structural analogues.
- To highlight recent advancements in drug delivery strategies targeting amino acid transporters, such as prodrugs and nanocarriers.
Main Methods:
- Review of existing literature on amino acid transporter expression in cancer.
- Analysis of transporter recognition mechanisms (acid-base properties, conformational isomerism, structural analogues).
- Examination of current drug delivery strategies, including prodrugs and nanocarriers, focusing on transporter-mediated endocytosis.
Main Results:
- Amino acid transporters show distinct expression patterns in cancer, correlating with tumor progression.
- Understanding transporter recognition is key to designing effective targeting agents.
- Prodrugs and nanocarriers show promise for targeted delivery via transporter-mediated endocytosis.
Conclusions:
- Amino acid transporters represent a significant target for innovative cancer therapies.
- Further research into transporter mechanisms and drug delivery systems can lead to more effective tumor-targeting strategies.
- Targeting amino acid transporters offers a promising avenue for enhancing the efficacy of cancer treatments.
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