Targeting galectin-4 with glycoconjugates of varying architectures: a multivalency étude with accent on anti-tumor effect and protection against apoptosis
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F25%3A00639544" target="_blank" >RIV/61388963:_____/25:00639544 - isvavai.cz</a>
Alternative codes found
RIV/61388971:_____/25:00639544 RIV/68407700:21460/25:00389989 RIV/00216208:11310/25:10503720
Result on the web
<a href="https://www.sciencedirect.com/science/article/pii/S0223523425009146?via%3Dihub" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0223523425009146?via%3Dihub</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.ejmech.2025.118149" target="_blank" >10.1016/j.ejmech.2025.118149</a>
Alternative languages
Result language
angličtina
Original language name
Targeting galectin-4 with glycoconjugates of varying architectures: a multivalency étude with accent on anti-tumor effect and protection against apoptosis
Original language description
Galectin-4 (Gal-4) is a protumorigenic protein that strongly participates especially in gastrointestinal cancer and is increasingly recognized as a therapeutic target in gastrointestinal malignancies, where its dysregulated expression contributes to tumor progression and immune modulation. Its abundance and the extent of its involvement in these pathologies are comparable with its much better-studied counterparts, galectin-1 and3. However, to date, no systematic effort has been made to design efficient defined Gal-4 inhibitors with a potential therapeutic effect. In this work, we present a library of biocompatible multivalent Gal-4 inhibitors with diverse architectures to investigate how different modes of multivalent presentation of a common ligand, lactose, influence the binding affinity to Gal-4. The most efficient scaffold was then loaded with a high-affinity tetrasaccharide ligand of Gal-4, derived from lacto-N-tetraose, to further enhance Gal-4 binding. The resulting glycopolymer exhibited outstanding performance in inhibiting Gal-4-induced apoptosis of T lymphocytes, and, in addition, it efficiently scavenged Gal-4 from the surface of cancer cells. Both of these processes are relevant for tumor immune evasion. Given the high biocompatibility, and low toxicity of the POx carrier, this glycopolymer has a strong potential as a candidate for further development of glycotherapeutics against Gal-4-associated diseases such as gastrointestinal cancer.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10406 - Analytical chemistry
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2025
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
European Journal of Medicinal Chemistry
ISSN
0223-5234
e-ISSN
1768-3254
Volume of the periodical
300
Issue of the periodical within the volume
15 Dec
Country of publishing house
FR - FRANCE
Number of pages
12
Pages from-to
118149
UT code for WoS article
001583014200001
EID of the result in the Scopus database
2-s2.0-105015645847