Galectins are soluble β‐D‐galactoside‐binding proteins whose implication in cancer progression and disease outcome makes them prominent targets for therapeutic intervention. In this frame, the development of small inhibitors that block selectively the activity of galectins represents an important strategy for cancer therapy which is, however, still relatively underdeveloped. To this end, we designed here a rationally and efficiently novel diglycosylated compound, characterized by a selenoglycoside bond and the presence of a lipophilic benzyl group at both saccharide residues. The relatively high binding affinity of the new compound to the carbohydrate recognition domain of two galectins, galectin 3 and galectin 9, its good antiproliferative and anti‐migration activity towards melanoma cells, as well as its anti‐angiogenesis properties, pave the way for its further development as an anticancer agent.

Design, Synthesis, and Anticancer Activity of a Selenium‐Containing Galectin‐3 and Galectin‐9N Inhibitor / Di Gaetano, S.; Pirone, L.; Galdadas, I.; Traboni, S.; Iadonisi, A.; Pedone, E.; Saviano, M.; Gervasio, F. L.; Capasso, D.. - In: INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES. - ISSN 1661-6596. - 23:5(2022), p. 2581. [10.3390/ijms23052581]

Design, Synthesis, and Anticancer Activity of a Selenium‐Containing Galectin‐3 and Galectin‐9N Inhibitor

Pirone L.;Traboni S.;Iadonisi A.;Saviano M.;Capasso D.
2022

Abstract

Galectins are soluble β‐D‐galactoside‐binding proteins whose implication in cancer progression and disease outcome makes them prominent targets for therapeutic intervention. In this frame, the development of small inhibitors that block selectively the activity of galectins represents an important strategy for cancer therapy which is, however, still relatively underdeveloped. To this end, we designed here a rationally and efficiently novel diglycosylated compound, characterized by a selenoglycoside bond and the presence of a lipophilic benzyl group at both saccharide residues. The relatively high binding affinity of the new compound to the carbohydrate recognition domain of two galectins, galectin 3 and galectin 9, its good antiproliferative and anti‐migration activity towards melanoma cells, as well as its anti‐angiogenesis properties, pave the way for its further development as an anticancer agent.
2022
Design, Synthesis, and Anticancer Activity of a Selenium‐Containing Galectin‐3 and Galectin‐9N Inhibitor / Di Gaetano, S.; Pirone, L.; Galdadas, I.; Traboni, S.; Iadonisi, A.; Pedone, E.; Saviano, M.; Gervasio, F. L.; Capasso, D.. - In: INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES. - ISSN 1661-6596. - 23:5(2022), p. 2581. [10.3390/ijms23052581]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/882500
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