Quadruplex-Forming Motif Inserted into 3 ' UTR of Ty1his3-AI Retrotransposon Inhibits Retrotransposition in Yeast

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68081707%3A_____%2F21%3A00542265" target="_blank" >RIV/68081707:_____/21:00542265 - isvavai.cz</a>
Result on the web
<a href="https://www.mdpi.com/2079-7737/10/4/347" target="_blank" >https://www.mdpi.com/2079-7737/10/4/347</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/biology10040347" target="_blank" >10.3390/biology10040347</a>

Result language
angličtina
Original language name
Quadruplex-Forming Motif Inserted into 3 ' UTR of Ty1his3-AI Retrotransposon Inhibits Retrotransposition in Yeast
Original language description
Current multiagent chemotherapy regimens have improved the cure rate in acute leukemia patients, but they are highly toxic and poorly efficient in relapsed patients. To improve the treatment approaches, new specific molecules are needed. The G-quadruplexes (G4s), which are noncanonical nucleic acid structures found in specific guanine-rich DNA or RNA, are involved in many cellular events, including control of gene expression. G4s are considered as targets for the development of anticancer agents. Heterocyclic molecules are well known to target and stabilize G4 structures. Thus, a new series of 2,9-bis[(substituted-aminomethyl)phenyl]-1,10-phenanthroline derivatives (1a-i) was designed, synthesized, and evaluated against five human myeloid leukemia cell lines (K562, KU812, MV4-11, HL60, and U937). Their ability to stabilize various oncogene promoter G4 structures (c-MYC, BCL-2, and K-RAS) as well as the telomeric G4 was also determined through the fluorescence resonance energy transfer melting assay and native mass spectrometry. In addition, the more bioactive ligands 1g-i were tested for telomerase activity in HuT78 and MV4-11 protein extracts.
Czech name
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Czech description
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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
10620 - Other biological topics

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

Publication year
2021
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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