Elevated levels of galectin-3 are associated with tumorigenesis. Its inhibition with high-affinity carbohydrate ligands opens new therapeutic routes. Targeting of intracellular galectin-3 is challenging for polar inhibitors like carbohydrates. We demonstrate the potential of novel biomedical research tools, glycocalix[4]arenes, to enter epithelial cells, which may allow their interaction with galectin-3.

Department of Analytical Chemistry Faculty of Science Charles University Prague Hlavova 8 CZ 12843 Praha 2 Czech Republic

Department of Health Care Disciplines and Population Protection Faculty of Biomedical Engineering Czech Technical University Prague nám Sítná 3105 CZ 27201 Kladno Czech Republic

Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences Flemingovo nám 2 CZ 16610 Praha 6 Czech Republic

Laboratory of Biotransformation Institute of Microbiology of the Czech Academy of Sciences Vídeňská 1083 CZ 14220 Praha 4 Czech Republic

University of Chemistry and Technology Prague Technická 5 CZ 16628 Praha 6 Czech Republic

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Glycopolymer Inhibitors of Galectin-3 Suppress the Markers of Tissue Remodeling in Pulmonary Hypertension