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小分子抑制葡萄糖转运蛋白 GLUT-1-4。

Small-Molecule Inhibition of Glucose Transporters GLUT-1-4.

机构信息

Department Chemical Biology, Max Planck Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.

Department Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.

出版信息

Chembiochem. 2020 Jan 15;21(1-2):45-52. doi: 10.1002/cbic.201900544. Epub 2019 Nov 8.

Abstract

Glucose addiction is observed in cancer and other diseases that are associated with hyperproliferation. The development of compounds that restrict glucose supply and decrease glycolysis has great potential for the development of new therapeutic approaches. Addressing facilitative glucose transporters (GLUTs), which are often upregulated in glucose-dependent cells, is therefore of particular interest. This article reviews a selection of potent, isoform-selective GLUT inhibitors and their biological characterization. Potential therapeutic applications of GLUT inhibitors in oncology and other diseases that are linked to glucose addiction are discussed.

摘要

葡萄糖成瘾现象存在于癌症和其他与过度增殖相关的疾病中。开发限制葡萄糖供应和降低糖酵解的化合物,对于开发新的治疗方法具有巨大的潜力。因此,针对在葡萄糖依赖性细胞中常被上调的易化型葡萄糖转运蛋白(GLUTs)具有特别的意义。本文综述了一系列具有高活性和对亚型具有选择性的 GLUT 抑制剂及其生物学特性。还讨论了 GLUT 抑制剂在肿瘤学和其他与葡萄糖成瘾相关的疾病中的潜在治疗应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d33d/7004114/4e87b7029160/CBIC-21-45-g003.jpg

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