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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

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • 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

  • 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