Discovery of new inhibitors of nuclease MRE11
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68378050%3A_____%2F25%3A00617707" target="_blank" >RIV/68378050:_____/25:00617707 - isvavai.cz</a>
Alternative codes found
RIV/00216224:14310/25:00140679 RIV/00159816:_____/25:00082273
Result on the web
<a href="https://doi.org/10.1016/j.ejmech.2024.117226" target="_blank" >https://doi.org/10.1016/j.ejmech.2024.117226</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.ejmech.2024.117226" target="_blank" >10.1016/j.ejmech.2024.117226</a>
Alternative languages
Result language
angličtina
Original language name
Discovery of new inhibitors of nuclease MRE11
Original language description
MRE11 nuclease is a central player in signaling and processing DNA damage, and in resolving stalled replication forks. Here, we describe the identification and characterization of new MRE11 inhibitors MU147 and MU1409. Both compounds inhibit MRE11 nuclease more specifically and effectively than the relatively weak state-of-theart inhibitor mirin. They also abrogate double-strand break repair mechanisms that rely on MRE11 nuclease activity, without impairing ATM activation. Inhibition of MRE11 also impairs nascent strand degradation of stalled replication forks and selectively affects BRCA2-deficient cells. Herein, we illustrate that our newly discovered compounds MU147 and MU1409 can be used as chemical probes to further explore the biological role of MRE11 and support the potential clinical relevance of pharmacological inhibition of this nuclease.
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
10608 - Biochemistry and molecular biology
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
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
European Journal of Medicinal Chemistry
ISSN
0223-5234
e-ISSN
1768-3254
Volume of the periodical
285
Issue of the periodical within the volume
5 March
Country of publishing house
FR - FRANCE
Number of pages
20
Pages from-to
117226
UT code for WoS article
001410134300001
EID of the result in the Scopus database
2-s2.0-85214325739