Cell-based DNA demethylation detection system for screening of epigenetic drugs in 2D, 3D, and xenograft models
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F17%3A00474988" target="_blank" >RIV/61388963:_____/17:00474988 - isvavai.cz</a>
Alternative codes found
RIV/61989592:15110/16:73585143
Result on the web
<a href="http://dx.doi.org/10.1002/cyto.a.23004" target="_blank" >http://dx.doi.org/10.1002/cyto.a.23004</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1002/cyto.a.23004" target="_blank" >10.1002/cyto.a.23004</a>
Alternative languages
Result language
angličtina
Original language name
Cell-based DNA demethylation detection system for screening of epigenetic drugs in 2D, 3D, and xenograft models
Original language description
Aberrant DNA methylation that results in silencing of genes has remained a significant interest in cancer research. Despite major advances, the success of epigenetic therapy is elusive due to narrow therapeutic window. A wide variety of naturally occurring epigenetic agents and synthetic molecules that can alter methylation patterns exist, however, their usefulness in epigenetic therapy remains unknown. This underlines the need for effective tumor models for large-scale screening of drug candidates with potent hypomethylation activity. In this study, we present the development of a cell-based DNA demethylation detection system, which is amenable for high content screening of epigenetic drugs in two-dimensional and three-dimensional cell culture models. Additionally, the detection system also supports the in vivo monitoring of demethylation efficacy of potential lead compounds from in vitro screens in tumor xenografts. The described detection system not only permits the continuous monitoring of demethylation but also of the induced cytostatic/cytotoxic drug effects in live cells, as a function of time. The detection system is fluorescence based and exploits the dominant ability of DNA methylation to inhibit gene transcription, and utilizes FLJ32130 gene, which is silenced on account of promoter hypermethylation in human colorectal cancer. The described work will provide the researchers with an efficient tool for epigenetic drug screens on a high throughput platform and would therefore benefit academic and industrial drug discovery.
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
10401 - Organic chemistry
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
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Cytometry. Part A
ISSN
1552-4922
e-ISSN
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Volume of the periodical
91A
Issue of the periodical within the volume
2
Country of publishing house
US - UNITED STATES
Number of pages
11
Pages from-to
133-143
UT code for WoS article
000395651800004
EID of the result in the Scopus database
2-s2.0-85006093161