Počet záznamů: 1
Glycopolymers Decorated with 3-O-Substituted Thiodigalactosides as Potent Multivalent Inhibitors of Galectin-3
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SYSNO ASEP 0556381 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Glycopolymers Decorated with 3-O-Substituted Thiodigalactosides as Potent Multivalent Inhibitors of Galectin-3 Tvůrce(i) Vrbata, David (MBU-M) ORCID
Filipová, Marcela (UMCH-V) RID, ORCID
Tavares, Marina Rodrigues (UMCH-V) ORCID, RID
Červený, Jakub (MBU-M) ORCID, RID
Vlachová, Miluše (MBU-M) ORCID
Šírová, Milada (MBU-M) RID, ORCID
Pelantová, Helena (MBU-M) ORCID, RID
Petrásková, Lucie (MBU-M) ORCID
Bumba, Ladislav (MBU-M) RID, ORCID
Konefal, Rafal (UMCH-V) RID, ORCID
Etrych, Tomáš (UMCH-V) RID, ORCID
Křen, Vladimír (MBU-M) RID, ORCID
Chytil, Petr (UMCH-V) RID, ORCID
Bojarová, Pavla (MBU-M) ORCIDZdroj.dok. Journal of Medicinal Chemistry. - : American Chemical Society - ISSN 0022-2623
Roč. 65, č. 5 (2022), s. 3866-3878Poč.str. 13 s. Jazyk dok. eng - angličtina Země vyd. US - Spojené státy americké Klíč. slova digit nm affinity ; high selectivity ; click chemistry ; copolymers ; glycopeptide ; recognition ; derivatives ; apoptosis ; fibrosis ; arginine Vědní obor RIV CE - Biochemie Obor OECD Biochemistry and molecular biology Vědní obor RIV – spolupráce Ústav makromolekulární chemie - Makromolekulární chemie CEP LTC19038 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy GA22-00262S GA ČR - Grantová agentura ČR NU21-03-00273 GA MZd - Ministerstvo zdravotnictví Způsob publikování Omezený přístup Institucionální podpora MBU-M - RVO:61388971 ; UMCH-V - RVO:61389013 UT WOS 000772205900011 EID SCOPUS 85125127905 DOI 10.1021/acs.jmedchem.1c01625 Anotace Galectin-3 (Gal-3) participates in many cancer-related metabolic processes. The inhibition of overexpressed Gal-3 by, e.g., beta-galactoside-derived inhibitors is hence promising for cancer treatment. The multivalent presentation of such inhibitors on a suitable biocompatible carrier can enhance the overall affinity to Gal-3 and favorably modify the interaction with Gal-3-over-expressing cells. We synthesized a library of C-3 aryl-substituted thiodigalactoside inhibitors and their multivalent N-(2-hydroxypropyl)methacrylamide (HPMA)-based counterparts with two different glycomimetic contents. Glycopolymers with a higher content of glycomimetic exhibited a higher affinity to Gal-3 as assessed by ELISA and biolayer interferometry. Among them, four candidates (with 4-acetophenyl, 4-cyanophenyl, 4-fluorophenyl, and thiophen-3-yl substitution) were selected for further evaluation in cancer-related experiments in cell cultures. These glycopolymers inhibited Gal-3-induced processes in cancer cells. The cyanophenyl-substituted glycopolymer exhibited the strongest antiproliferative, antimigratory, antiangiogenic, and immunoprotective properties. The prepared glycopolymers appear to be prospective modulators of the tumor microenvironment applicable in the therapy of Gal-3-associated cancers. Pracoviště Mikrobiologický ústav Kontakt Eliška Spurná, eliska.spurna@biomed.cas.cz, Tel.: 241 062 231 Rok sběru 2023 Elektronická adresa https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01625
Počet záznamů: 1