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. 2016 Dec;33(6):853-876.
doi: 10.1007/s10719-016-9721-z. Epub 2016 Aug 15.

Synthetic Glycoconjugates Inhibitors of Tumor-Related galectin-3: An Update


Synthetic Glycoconjugates Inhibitors of Tumor-Related galectin-3: An Update

Vanessa Leiria Campo et al. Glycoconj J. .


Galectin-3 is associated with the development and malignancy of several types of tumor, mediating important tumor-related functions, such as tumorigenesis, neoplastic transformation, tumor cell survival, angiogenesis, tumor metastasis and regulation of apoptosis. Therefore, synthetic galectin-3 inhibitors are of utmost importance for development of new antitumor therapeutic strategies. In this review we present an updated selection of synthetic glycoconjugates inhibitors of tumor-related galectin-3, properly addressed as monosaccharide- and disaccharide-based inhibitors, and multivalent-based inhibitors, disclosuring relevant methods for their synthesis along with their inhibitory activities towards galectin-3. In general, Cu(I)-assisted 1,3-dipolar azide-alkyne cycloaddition (CuAAC) reactions were predominantly applied for the synthesis of the described inhibitors, which had their inhibitory activities against galectin-3 evaluated by fluorescence polarization, surface plasmon resonance (SPR), hemagglutination, ELISA and cell imaging assays. Overall, the presented synthetic glycoconjugates represent frontline galectin-3 inhibitors, finding important biomedical applications in cancer.

Keywords: Disaccharides; Galectin-3; Glycoconjugates; Monosaccharides; Multivalent-based inhibitors; Tumor.

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