Identification of Eukaryotic Translation Elongation Factor 1-alpha 1 Gamendazole-Binding Site for Binding of 3-Hydroxy-4(1&ITH&IT)-quinolinones as Novel Ligands with Anticancer Activity
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11130%2F18%3A10375275" target="_blank" >RIV/00216208:11130/18:10375275 - isvavai.cz</a>
Result on the web
<a href="https://doi.org/10.1021/acs.jmedchem.8b00078" target="_blank" >https://doi.org/10.1021/acs.jmedchem.8b00078</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/acs.jmedchem.8b00078" target="_blank" >10.1021/acs.jmedchem.8b00078</a>
Alternative languages
Result language
angličtina
Original language name
Identification of Eukaryotic Translation Elongation Factor 1-alpha 1 Gamendazole-Binding Site for Binding of 3-Hydroxy-4(1&ITH&IT)-quinolinones as Novel Ligands with Anticancer Activity
Original language description
Here, we have identified the interaction site of the contraceptive drug gamendazole using computational modeling. The drug was previously described as a ligand for eukaryotic translation elongation factor 1-alpha 1 (eEF1A1) and found to be a potential target site for derivatives of 2-phenyl-3-hydroxy-4(1H)-quinolinones (3-HQs), which exhibit anticancer activity. The interaction of this class of derivatives of 3-HQs with eEF1A1 inside cancer cells was confirmed via pull-down assay. We designed and synthesized a new family of 3-HQs and subsequently applied isothermal titration calorimetry to show that these compounds strongly bind to eEF1A1. Further, we found that some of these derivatives possess significant in vitro anticancer activity.
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
S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2018
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Journal of Medicinal Chemistry
ISSN
0022-2623
e-ISSN
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Volume of the periodical
61
Issue of the periodical within the volume
7
Country of publishing house
US - UNITED STATES
Number of pages
10
Pages from-to
3027-3036
UT code for WoS article
000430256600026
EID of the result in the Scopus database
2-s2.0-85045569345