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      Novel strategies to improve tumour therapy by targeting the proteins MCT1, MCT4 and LAT1.

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          Abstract

          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.

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          Author and article information

          Journal
          Eur J Med Chem
          European journal of medicinal chemistry
          Elsevier BV
          1768-3254
          0223-5234
          Dec 15 2021
          : 226
          Affiliations
          [1 ] Personnel Department, Guang Xi University of Chinese Medicine, Nanning, 530200, PR China.
          [2 ] School of Pharmacy, Guang Xi University of Chinese Medicine, Nanning, 530200, PR China.
          [3 ] Zhuang Yao Medicine Center of Engineering and Technology, Guang Xi University of Chinese Medicine, Nanning, 530200, PR China.
          [4 ] Key Laboratory of Structure-Based Drug Design and Discovery, Shenyang Pharmaceutical University, Ministry of Education, China.
          [5 ] Zhuang Yao Medicine Center of Engineering and Technology, Guang Xi University of Chinese Medicine, Nanning, 530200, PR China. Electronic address: wanggang_521521@163.com.
          Article
          S0223-5234(21)00655-3
          10.1016/j.ejmech.2021.113806
          34517305
          74f7d963-d5d6-4818-ab1e-6a6569913415
          History

          l-type amino acid transporter 1,4,Mono-carboxylate transporter1,Tumour therapy

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