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Chemosensitization of tumors via simultaneous delivery of STAT3 inhibitor and doxorubicin through HPMA copolymer-based nanotherapeutics with pH-sensitive activation.
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SYSNO ASEP 0580702 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Chemosensitization of tumors via simultaneous delivery of STAT3 inhibitor and doxorubicin through HPMA copolymer-based nanotherapeutics with pH-sensitive activation. Tvůrce(i) Kovář, Marek (MBU-M) RID, ORCID
Šubr, Vladimír (UMCH-V) RID, ORCID
Běhalová, Kateřina (MBU-M)
Studenovský, Martin (UMCH-V) RID, ORCID
Starenko, Daniil (MBU-M)
Kovářová, Jiřina (MBU-M)
Procházková, Petra (MBU-M) RID, ORCID
Etrych, Tomáš (UMCH-V) RID, ORCID
Kostka, Libor (UMCH-V) RID, ORCIDZdroj.dok. Nanomedicine: Nanotechnology, Biology and Medicine. - : Elsevier - ISSN 1549-9634
Roč. 56, February 2024 (2024), s. 102730Poč.str. 15 s. Jazyk dok. eng - angličtina Země vyd. NL - Nizozemsko Klíč. slova STAT3 inhibitor ; Doxorubicin ; HPMA copolymer carrier ; pH-sensitive drug ; release Obor OECD Pharmacology and pharmacy CEP NU21-03-00273 GA MZd - Ministerstvo zdravotnictví LX22NPO5102 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy Způsob publikování Open access Institucionální podpora MBU-M - RVO:61388971 ; UMCH-V - RVO:61389013 UT WOS 38158146 DOI 10.1016/j.nano.2023.102730 Anotace We synthesized three novel STAT3 inhibitors (S3iD1-S3iD3) possessing oxoheptanoic residue enabling linkage to HPMA copolymer carrier via a pH-sensitive hydrazone bond. HPMA copolymer conjugates bearing doxorubicin (Dox) and our STAT3 inhibitors were synthesized to evaluate the anticancer effect of Dox and STAT3 inhibitor co-delivery into tumors. S3iD1-3 and their copolymer-bound counterparts (P-S3iD1-P-S3iD3) showed considerable in vitro cytostatic activities in five mouse and human cancer cell lines with IC50 ~0.6-7.9 muM and 0.7-10.9 muM, respectively. S3iD2 and S3iD3 were confirmed to inhibit the STAT3 signaling pathway. The combination of HPMA copolymer-bound Dox (P-Dox) and P-S3iD3 at the dosage showing negligible toxicity demonstrated significant antitumor activity in B16F10 melanoma-bearing mice and completely cured 2 out of 15 mice. P-Dox alone had a significantly lower therapeutic activity with no completely cured mice. Thus, polymer conjugates bearing STAT3 inhibitors may be used for the chemosensitization of chemorefractory tumors. Pracoviště Mikrobiologický ústav Kontakt Eliška Spurná, eliska.spurna@biomed.cas.cz, Tel.: 241 062 231 Rok sběru 2025 Elektronická adresa https://www.sciencedirect.com/science/article/pii/S1549963423000813
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