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探索单羧酸转运体抑制作用用于癌症治疗。

Exploring monocarboxylate transporter inhibition for cancer treatment.

作者信息

Koltai Tomas, Fliegel Larry

机构信息

Hospital del Centro Gallego de Buenos Aires, Buenos Aires 2199, Argentina.

Department of Biochemistry, Faculty of Medicine, University of Alberta, Edmonton T6G 2R3, Alberta, Canada.

出版信息

Explor Target Antitumor Ther. 2024;5(1):135-169. doi: 10.37349/etat.2024.00210. Epub 2024 Feb 23.

DOI:10.37349/etat.2024.00210
PMID:38464385
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10918235/
Abstract

Cells are separated from the environment by a lipid bilayer membrane that is relatively impermeable to solutes. The transport of ions and small molecules across this membrane is an essential process in cell biology and metabolism. Monocarboxylate transporters (MCTs) belong to a vast family of solute carriers (SLCs) that facilitate the transport of certain hydrophylic small compounds through the bilipid cell membrane. The existence of 446 genes that code for SLCs is the best evidence of their importance. In-depth research on MCTs is quite recent and probably promoted by their role in cancer development and progression. Importantly, it has recently been realized that these transporters represent an interesting target for cancer treatment. The search for clinically useful monocarboxylate inhibitors is an even more recent field. There is limited pre-clinical and clinical experience with new inhibitors and their precise mechanism of action is still under investigation. What is common to all of them is the inhibition of lactate transport. This review discusses the structure and function of MCTs, their participation in cancer, and old and newly developed inhibitors. Some suggestions on how to improve their anticancer effects are also discussed.

摘要

细胞通过对溶质相对不通透的脂质双分子层膜与外界环境分隔开来。离子和小分子跨膜运输是细胞生物学和新陈代谢中的一个重要过程。单羧酸转运体（MCTs）属于庞大的溶质载体（SLCs）家族，可促进某些亲水性小分子化合物通过双脂细胞膜进行运输。有446个编码SLCs的基因存在，这是它们重要性的最佳证据。对MCTs的深入研究是最近才开展的，可能是由于它们在癌症发生和发展中的作用所推动。重要的是，最近人们认识到这些转运体是癌症治疗的一个有趣靶点。寻找临床上有用的单羧酸抑制剂是一个更新的领域。新型抑制剂的临床前和临床经验有限，其确切作用机制仍在研究中。它们的共同之处在于抑制乳酸运输。本文综述了MCTs的结构和功能、它们在癌症中的作用以及新老抑制剂。还讨论了一些关于如何提高其抗癌效果的建议。

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