Fluorescence Detection of DNA/RNA G-Quadruplexes (G4s) by Twice-as-Smart Ligands
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22310%2F25%3A43930592" target="_blank" >RIV/60461373:22310/25:43930592 - isvavai.cz</a>
Result on the web
<a href="https://chemistry-europe.onlinelibrary.wiley.com/doi/full/10.1002/cmdc.202400829" target="_blank" >https://chemistry-europe.onlinelibrary.wiley.com/doi/full/10.1002/cmdc.202400829</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1002/cmdc.202400829" target="_blank" >10.1002/cmdc.202400829</a>
Alternative languages
Result language
angličtina
Original language name
Fluorescence Detection of DNA/RNA G-Quadruplexes (G4s) by Twice-as-Smart Ligands
Original language description
Fluorescence detection of DNA and RNA G-quadruplexes (G4s) is a very efficient strategy to assess not only the existence and prevalence of cellular G4s but also their relevance as targets for therapeutic interventions. Among the fluorophores used to this end, turn-on probes are the most interesting since their fluorescence is triggered only upon interaction with their G4 targets, which ensures a high sensitivity and selectivity of detection. We reported on a series of twice-as-smart G4 probes, which are both smart G4 ligands (whose structure is reorganized upon interaction with G4s) and smart fluorescent probes (whose fluorescence is turned on upon interaction with G4s). The fine mechanistic details behind the excellent properties of the best prototype N-TASQ remain to be deciphered: to investigate this, we report here on the synthesis and studies of two analogues, TzN-TASQ and AlkN-TASQ, and on a careful analysis of their G4-interacting properties, investigated both in vitro and in silico. Our results show that fine-tuning their constitutive structural elements allows for increasing the efficiency of both their 'off' (i. e., a conformation with a low fluorescence) and 'on' states (i. e., a conformation with a high fluorescence), which opens interesting ways for the design of more efficient fluorogenic G4 probes.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30107 - Medicinal chemistry
Result continuities
Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2025
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
ChemMedChem
ISSN
1860-7179
e-ISSN
1860-7187
Volume of the periodical
20
Issue of the periodical within the volume
7
Country of publishing house
TW - TAIWAN (PROVINCE OF CHINA)
Number of pages
8
Pages from-to
"e202400829"
UT code for WoS article
001396682000001
EID of the result in the Scopus database
2-s2.0-85214794270