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Article
Fast Responding Genes to HIF Prolyl Hydroxylase Inhibitors
The attempts to elucidate the mechanism of the hypoxic activation of erythropoietin synthesis lead to the discovery of the hypoxia inducible factor (HIF) and its stability regulation via HIF prolyl hydroxylase...
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Article
Transport and toxicity of 5-fluorouracil, doxorubicin, and cyclophosphamide in in vitro placental barrier model based on BeWo b30 cells
An in vitro placental barrier model based on human choriocarcinoma BeWo b30 cell line was considered as a method of preclinical study of the transport and toxicity of antitumor agents and other organic compounds....
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Article
Quantitative Analysis of Cell-Based Luciferase Fusion Reporters
Cell-based reporters expressing luciferase fusions with transcription factors or their protein stability domains can be considered as microbioreactors providing a way to directly monitor the stability of the l...
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Article
Structural optimization of adaptaquin, a HIF prolyl hydroxylase inhibitor
The structural optimization of adaptaquin, viz., 7-(4-chlorophenyl)[(3-hydroxypyridin-2-yl)amino]methylquinolin-8-ol, a HIF (hypoxia inducible factor) prolyl hydroxylase inhibitor, was carried out. This was done ...
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Article
Antihypoxic activity of adaptaquin enantiomers
Adaptaquin, 7-{(4-chlorophenyl)[(3-hydroxypyridin-2-yl)amino]methyl}quinolin-8-ol (1), was identified in our earlier study as a hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor by high-throughput scree...
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Article
Metal Ions as Activators of Hypoxia Inducible Factor
Activation of antihypoxic program under the action of a number of transition and heavy metals has been studied using cell-based HIF1 ODD-luc and HRE-luc reporters. It has been demonstrated that Au3+, Pb2+, Sn2+, ...
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Article
HIF2 ODD-luciferase reporter: the most sensitive assay for HIF prolyl hydroxylase inhibitors
Reporters expressing fusion proteins of HIF2 and HIF3 C-terminal oxygen degradable domain (ODD) with the firefly luciferase, HIF2 ODD-luc and HIF3 ODD-luc, were constructed and briefly characterized. Stable ne...
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Article
Antioxidant and antihypoxic properties of neuroprotective drugs
The screening of the library containing 320 drugs and biologically active compounds was carried out. The library was created for testing potent agents on Rett syndrome models (SMART library) using new-generati...