Počet záznamů: 1
Lysosome-Targeting Amplifiers of Reactive Oxygen Species as Anticancer Prodrugs
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SYSNO ASEP 0485730 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Lysosome-Targeting Amplifiers of Reactive Oxygen Species as Anticancer Prodrugs Tvůrce(i) Daum, S. (DE)
Reshetnikov, M.S.V. (DE)
Šíša, Miroslav (UEB-Q) ORCID
Dumych, T. (UA)
Lootsik, M. D. (UA)
Bilyy, R. (UA)
Bila, E. (UA)
Janko, C. (DE)
Alexiou, C. (DE)
Herrmann, M. (DE)
Sellner, L. (DE)
Mokhir, A. (DE)Celkový počet autorů 12 Zdroj.dok. Angewandte Chemie - International Edition. - : Wiley - ISSN 1433-7851
Roč. 56, č. 49 (2017), s. 15545-15549Poč.str. 5 s. Jazyk dok. eng - angličtina Země vyd. DE - Německo Klíč. slova aminoferrocene ; cancer ; lysosomes ; prodrugs ; reactive oxygen species Vědní obor RIV ED - Fyziologie Obor OECD Organic chemistry Institucionální podpora UEB-Q - RVO:61389030 UT WOS 000416244200006 EID SCOPUS 85033445233 DOI 10.1002/anie.201706585 Anotace Cancer cells produce elevated levels of reactive oxygen species, which has been used to design cancer specific prodrugs. Their activation relies on at least a bimolecular process, in which a prodrug reacts with ROS. However, at low micromolar concentrations of the prodrugs and ROS, the activation is usually inefficient. Herein, we propose and validate a potentially general approach for solving this intrinsic problem of ROS-dependent prodrugs. In particular, known prodrug 4-(N-ferrocenyl-N-benzylaminocarbonyloxymethyl)phenylboronic acid pinacol ester was converted into its lysosome-specific analogue. Since lysosomes contain a higher concentration of active ROS than the cytoplasm, activation of the prodrug was facilitated with respect to the parent compound. Moreover, it was found to exhibit high anticancer activity in a variety of cancer cell lines (IC 50 =3.5–7.2 μm) and in vivo (40 mg kg −1 , NK/Ly murine model) but remained weakly toxic towards non-malignant cells (IC 50 =15–30 μm). Pracoviště Ústav experimentální botaniky Kontakt David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Rok sběru 2018
Počet záznamů: 1