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Published on: July 12, 2018
Synthetic glycoconjugates inhibitors of tumor-related galectin-3: an update
Vanessa Leiria Campo1, Marcelo Fiori Marchiori2, Lílian Cataldi Rodrigues2
1Faculdade de Ciências Farmacêuticas de Ribeirão Preto, USP, Av. Café S/N, CEP, Ribeirão Preto, SP, 14040-903, Brazil. vlcampo@fcfrp.usp.br.
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.
Insights
Synthetic glycoconjugates targeting galectin-3 show promise as novel anticancer agents. These compounds, synthesized using methods like CuAAC, offer new therapeutic strategies for various tumors.
Area of Science:
- Biochemistry
- Medicinal Chemistry
- Oncology
Background:
- Galectin-3 is implicated in tumor development, malignancy, and metastasis.
- Targeting galectin-3 is crucial for developing new antitumor therapies.
Purpose of the Study:
- To review synthetic glycoconjugate inhibitors of tumor-associated galectin-3.
- To highlight synthesis methods and inhibitory activities of these compounds.
Main Methods:
- Predominant use of Copper(I)-catalyzed 1,3-dipolar azide-alkyne cycloaddition (CuAAC) reactions for synthesis.
- Evaluation of inhibitory activities using fluorescence polarization, SPR, hemagglutination, ELISA, and cell imaging assays.
Main Results:
- An updated selection of monosaccharide-, disaccharide-, and multivalent-based galectin-3 inhibitors is presented.
- The synthetic glycoconjugates demonstrate significant inhibitory activity against galectin-3.
Conclusions:
- Synthetic glycoconjugates are effective frontline inhibitors of galectin-3.
- These inhibitors hold significant biomedical applications in cancer therapy.
