Helquat dyes targeting G-quadruplexes as a new class of anti-HIV-1 inhibitors
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F23%3A00571224" target="_blank" >RIV/61388963:_____/23:00571224 - isvavai.cz</a>
Result on the web
<a href="https://doi.org/10.1038/s41598-023-33263-3" target="_blank" >https://doi.org/10.1038/s41598-023-33263-3</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1038/s41598-023-33263-3" target="_blank" >10.1038/s41598-023-33263-3</a>
Alternative languages
Result language
angličtina
Original language name
Helquat dyes targeting G-quadruplexes as a new class of anti-HIV-1 inhibitors
Original language description
The secondary structure of nucleic acids containing quartets of guanines, termed G-quadruplexes, is known to regulate the transcription of many genes. Several G-quadruplexes can be formed in the HIV-1 long terminal repeat promoter region and their stabilization results in the inhibition of HIV-1 replication. Here, we identified helquat-based compounds as a new class of anti-HIV-1 inhibitors that inhibit HIV-1 replication at the stage of reverse transcription and provirus expression. Using Taq polymerase stop and FRET melting assays, we have demonstrated their ability to stabilize G-quadruplexes in the HIV-1 long-terminal repeat sequence. Moreover, these compounds were not binding to the general G-rich region, but rather to G-quadruplex-forming regions. Finally, docking and molecular dynamics calculations indicate that the structure of the helquat core greatly affects the binding mode to the individual G-quadruplexes. Our findings can provide useful information for the further rational design of inhibitors targeting G-quadruplexes in HIV-1.
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
10607 - Virology
Result continuities
Project
<a href="/en/project/LX22NPO5103" target="_blank" >LX22NPO5103: National Institute of Virology and Bacteriology</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2023
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Scientific Reports
ISSN
2045-2322
e-ISSN
2045-2322
Volume of the periodical
13
Issue of the periodical within the volume
April
Country of publishing house
US - UNITED STATES
Number of pages
13
Pages from-to
6096
UT code for WoS article
000984454500085
EID of the result in the Scopus database
2-s2.0-85152381657