Publications by authors named "Andrey I Osipyants"
Article Synopsis
- This study compares the effectiveness of 2-oxoglutarate mimetics and branched-tail oxyquinoline inhibitors in activating HIF prolyl hydroxylase, focusing on their performance in a luciferase reporter assay.
- Novel oxyquinoline inhibitors identified in this research showed significantly higher potency than existing drugs like roxadustat and vadadustat, especially when 2-methyl substitution was applied.
- Transcriptomic analysis revealed that the new inhibitors stimulated HIF1 and HIF2 pathways similarly to roxadustat but had distinct effects on alternative pathways involving p53 and NF-κB, suggesting a specific action of the 2-methyl variant on HIF PHD2.
Epigenetic alterations represent promising therapeutic targets in cancer treatment. Recently it was revealed that small molecules have the potential to act as microRNA silencers. Capacity to bind the discrete stem-looped structure of pre-miR-21 and prevent its maturation opens opportunities to utilize such compounds for the prevention of initiation, progression, and chemoresistance of cancer.
View Article and Find Full Text PDFL-Ascorbate (L-Asc), but not D-isoascorbate (D-Asc) and N-acetylcysteine (NAC) suppress HIF1 ODD-luc reporter activation induced by various inhibitors of HIF prolyl hydroxylase (PHD). The efficiency of suppression by L-Asc was sensitive to the nature of HIF PHD inhibitor chosen for reporter activation. In particular, the inhibitors developed to compete with alpha-ketoglutarate (αKG), were less sensitive to suppression by the physiological range of L-Asc (40-100 μM) than those having a strong iron chelation motif.
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