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Published on: July 12, 2018
Synthetic inhibitors of galectin-1 and -3 selectively modulate homotypic cell aggregation and tumor cell apoptosis
Ida Iurisci1, Albana Cumashi, Andrei A Sherman
1Department of Oncology and Neurosciences, Foundation University G. D'Annunzio Chieti-Pescara, Italy.
Background:
Galectins have emerged as critical regulators of tumor progression and metastasis, by modulating different biological events including homotypic cell aggregation, apoptosis, migration, angiogenesis and immune escape. Therefore, galectin inhibitors might represent novel therapeutic agents for cancer.
Materials And Methods:
A series of structural analogs of the disaccharide methyl beta-lactosaminide were screened as potential galectin inhibitors by examining their capability to block binding of galectin-1 and/or galectin-3 to LGalS3BP in solid-phase assays. To demonstrate any functional role in vitro, oligosaccharides were characterized by their ability to regulate tumor cell apoptosis and LGalS3BP-induced homotypic cell aggregation.
Results:
Oligosaccharides differentially inhibited binding of each galectin to LGalS3BP. Compounds containing longer oligosaccharide chains were found to be potent inhibitors of both galectins under static conditions. Strikingly, the most active compound in inhibiting homotypic cell aggregation and tumor cell apoptosis was found to be allyl lactoside, which paradoxically exhibited a modest inhibitory capacity for blocking galectin-1 and -3 binding to LGalS3BP.
Conclusion:
Allyl lactoside represents a novel powerful inhibitor of tumor-associated homotypic cell aggregation and apoptosis. Further investigations are required to remodel selective and potent inhibitors capable of specifically modulating the activity of different members of the galectin family.
Insights
Allyl lactoside effectively inhibits tumor cell aggregation and apoptosis, crucial processes in cancer metastasis. This novel galectin inhibitor shows promise as a therapeutic agent for cancer treatment.
Area of Science:
- Biochemistry
- Molecular Biology
- Cancer Research
Background:
- Galectins regulate key cancer processes like metastasis, apoptosis, and immune escape.
- Galectin inhibitors are potential therapeutic agents for cancer treatment.
Purpose of the Study:
- To screen structural analogs of methyl beta-lactosaminide as galectin inhibitors.
- To evaluate the functional role of oligosaccharides in regulating tumor cell apoptosis and homotypic cell aggregation.
Main Methods:
- Screening of oligosaccharide analogs for inhibition of galectin-1 and galectin-3 binding to LGalS3BP.
- In vitro characterization of oligosaccharides for their ability to modulate tumor cell apoptosis and LGalS3BP-induced homotypic cell aggregation.
Main Results:
- Oligosaccharides showed differential inhibition of galectin binding to LGalS3BP.
- Longer oligosaccharide chains were potent inhibitors under static conditions.
- Allyl lactoside strongly inhibited homotypic cell aggregation and tumor cell apoptosis, despite modest binding inhibition.
Conclusions:
- Allyl lactoside is a novel inhibitor of tumor-associated homotypic cell aggregation and apoptosis.
- Further research is needed to develop selective galectin inhibitors for specific family members.
