title: Synthetic glycoconjugates inhibitors of tumor-related galectin-3: an update.
abstract: 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.
authors.affiliation: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, USP, Av. Café S/N, CEP, Ribeirão Preto, SP, 14040-903, Brazil. vlcampo@fcfrp.usp.br.
authors.forename: Vanessa Leiria
authors.initials: VL
authors.lastname: Campo
authors.affiliation: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, USP, Av. Café S/N, CEP, Ribeirão Preto, SP, 14040-903, Brazil.
authors.forename: Marcelo Fiori
authors.initials: MF
authors.lastname: Marchiori
authors.affiliation: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, USP, Av. Café S/N, CEP, Ribeirão Preto, SP, 14040-903, Brazil.
authors.forename: Lílian Cataldi
authors.initials: LC
authors.lastname: Rodrigues
authors.affiliation: Faculdade de Ciências Farmacêuticas de Ribeirão Preto, USP, Av. Café S/N, CEP, Ribeirão Preto, SP, 14040-903, Brazil.
authors.forename: Marcelo
authors.initials: M
authors.lastname: Dias-Baruffi
mesh_terms: D000818:Animals; D001798:Blood Proteins; D037502:Galectin 3 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D037161:Galectins; D006001:Glycoconjugates / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism
chemical_list: D001798:Blood Proteins; D037502:Galectin 3; D037161:Galectins; D006001:Glycoconjugates; C428445:LGALS3 protein, human; D009363:Neoplasm Proteins
keywords: Disaccharides; Galectin-3; Glycoconjugates; Monosaccharides; Multivalent-based inhibitors; Tumor