Glycopolymers for efficient inhibition of galectin-3: in vitro proof of efficacy using suppression of T lymphocyte apoptosis and tumor cell migration
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388971%3A_____%2F20%3A00531504" target="_blank" >RIV/61388971:_____/20:00531504 - isvavai.cz</a>
Alternative codes found
RIV/61389013:_____/20:00531504 RIV/68407700:21460/20:00348816
Result on the web
<a href="https://pubs.acs.org/doi/10.1021/acs.biomac.0c00515" target="_blank" >https://pubs.acs.org/doi/10.1021/acs.biomac.0c00515</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/acs.biomac.0c00515" target="_blank" >10.1021/acs.biomac.0c00515</a>
Alternative languages
Result language
angličtina
Original language name
Glycopolymers for efficient inhibition of galectin-3: in vitro proof of efficacy using suppression of T lymphocyte apoptosis and tumor cell migration
Original language description
The development of efficient galectin-3 (Gal-3) inhibitors draws attention in the field of anti-cancer therapy, especially due to the prominent role of extra- and intracellular Gal-3 in vital processes of cancerogenesis, such as immunosuppression, stimulation of tumor cells proliferation, survival, invasion, apoptotic resistance, and metastasis formation and progression. Here, by combining poly-LacNAc (Galβ4GlcNAc)-derived oligosaccharides with N-(2-hydroxypropyl) methacrylamide (HPMA) copolymers, we synthesized multivalent glycopolymer inhibitors with a high potential to target extracellular and intracellular Gal-3. The inhibitory capabilities of the best conjugate in the studied series were in the nanomolar range proving the excellent Gal-3 inhibitory potential. Moreover, thorough investigation of the inhibitory effect in the biological conditions showed that the glycopolymers strongly inhibited Gal-3-induced apoptosis of T lymphocytes and suppressed migration and spreading of colorectal, breast, melanoma, and prostate cancer cells. In sum, the strong inhibitory activity toward Gal-3, combined with favorable pharmacokinetics of HPMA copolymers ensuring enhanced tumor accumulation via the enhanced permeability and retention effect, nominate the glycopolymers containing LacdiNAc-LacNAc (GalNAcβ4GlcNAcβ3Galβ4GlcNAc) tetrasaccharide as promising tools for preclinical in anti-cancer therapy evaluation.
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
10404 - Polymer science
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
2020
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Biomacromolecules
ISSN
1525-7797
e-ISSN
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Volume of the periodical
21
Issue of the periodical within the volume
8
Country of publishing house
US - UNITED STATES
Number of pages
12
Pages from-to
3122-3133
UT code for WoS article
000562121800015
EID of the result in the Scopus database
2-s2.0-85089190797