UCL Discovery
UCL home » Library Services » Electronic resources » UCL Discovery

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; ... Capasso, D; + view all (2022) Design, Synthesis, and Anticancer Activity of a Selenium‐Containing Galectin‐3 and Galectin‐9N Inhibitor. International Journal of Molecular Sciences , 23 (5) , Article 2581. 10.3390/ijms23052581. Green open access

[thumbnail of Gervasio_Design, Synthesis, and Anticancer Activity of a Selenium Containing Galectin 3 and Galectin 9N Inhibitor_VoR.pdf]
Preview
Text
Gervasio_Design, Synthesis, and Anticancer Activity of a Selenium Containing Galectin 3 and Galectin 9N Inhibitor_VoR.pdf - Published Version

Download (3MB) | Preview

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.

Type: Article
Title: Design, Synthesis, and Anticancer Activity of a Selenium‐Containing Galectin‐3 and Galectin‐9N Inhibitor
Open access status: An open access version is available from UCL Discovery
DOI: 10.3390/ijms23052581
Publisher version: https://doi.org/10.3390/ijms23052581
Language: English
Additional information: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited
Keywords: galectin; digalactoside compounds; drug design; binding affinity melanoma cells
UCL classification: UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences > Dept of Chemistry
UCL > Provost and Vice Provost Offices > UCL BEAMS
UCL
URI: https://discovery.ucl.ac.uk/id/eprint/10145237
Downloads since deposit
56Downloads
Download activity - last month
Download activity - last 12 months
Downloads by country - last 12 months

Archive Staff Only

View Item View Item