Počet záznamů: 1
Towards Profiling of the G-Quadruplex Targeting Drugs in the Living Human Cells Using NMR Spectroscopy
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SYSNO ASEP 0555334 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Towards Profiling of the G-Quadruplex Targeting Drugs in the Living Human Cells Using NMR Spectroscopy Tvůrce(i) Krafčík, D. (CZ)
Istvankova, E. (CZ)
Dzatko, S. (CZ)
Viskova, P. (CZ)
Foldynová-Trantírková, Silvie (BFU-R) ORCID
Trantírek, L. (CZ)Celkový počet autorů 6 Číslo článku 6042 Zdroj.dok. International Journal of Molecular Sciences. - : MDPI
Roč. 22, č. 11 (2021)Poč.str. 14 s. Forma vydání Online - E Jazyk dok. eng - angličtina Země vyd. CH - Švýcarsko Klíč. slova structures in-vitro ; human telomere ; nucleic-acids ; dna ; rna ; ligands Obor OECD Biochemistry and molecular biology CEP EF15_003/0000477 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy Způsob publikování Open access Institucionální podpora BFU-R - RVO:68081707 UT WOS 000660126000001 EID SCOPUS 85107286658 DOI 10.3390/ijms22116042 Anotace Recently, the H-1-detected in-cell NMR spectroscopy has emerged as a unique tool allowing the characterization of interactions between nucleic acid-based targets and drug-like molecules in living human cells. Here, we assess the application potential of H-1 and F-19-detected in-cell NMR spectroscopy to profile drugs/ligands targeting DNA G-quadruplexes, arguably the most studied class of anti-cancer drugs targeting nucleic acids. We show that the extension of the original in-cell NMR approach is not straightforward. The severe signal broadening and overlap of H-1 in-cell NMR spectra of polymorphic G-quadruplexes and their complexes complicate their quantitative interpretation. Nevertheless, the H-1 in-cell NMR can be used to identify drugs that, despite strong interaction in vitro, lose their ability to bind G-quadruplexes in the native environment. The in-cell NMR approach is adjusted to a recently developed 3,5-bis(trifluoromethyl)phenyl probe to monitor the intracellular interaction with ligands using F-19-detected in-cell NMR. The probe allows dissecting polymorphic mixture in terms of number and relative populations of individual G-quadruplex species, including ligand-bound and unbound forms in vitro and in cellulo. Despite the probe's discussed limitations, the F-19-detected in-cell NMR appears to be a promising strategy to profile G-quadruplex-ligand interactions in the complex environment of living cells. Pracoviště Biofyzikální ústav Kontakt Jana Poláková, polakova@ibp.cz, Tel.: 541 517 244 Rok sběru 2022 Elektronická adresa https://www.mdpi.com/1422-0067/22/11/6042
Počet záznamů: 1