furan- and thiophene-2-carbonyl amino acid derivatives activate hypoxia-inducible factor via inhibition of factor inhibiting hypoxia-inducible factor-1

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ID: 163177
2018
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Ranked #165 of 1,185 articles by views in Journal of ethnopharmacology

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Abstrak
Induction of a series of anti-hypoxic proteins protects cells during exposure to hypoxic conditions. Hypoxia-inducible factor-α (HIF-α) is a major transcription factor that orchestrates this protective effect. To activate HIF exogenously, without exposing cells to hypoxic conditions, many small-molecule inhibitors targeting prolyl hydroxylase domain-containing protein have been developed. In addition, suppression of factor inhibiting HIF-1 (FIH-1) has also been shown to have the potential to activate HIF-α. However, few small-molecule inhibitors of FIH-1 have been developed. In this study, we synthesized a series of furan- and thiophene-2-carbonyl amino acid derivatives having the potential to inhibit FIH-1. The inhibitory activities of these compounds were evaluated in SK-N-BE(2)c cells by measuring HIF response element (HRE) promoter activity. Several furan- and thiophene-2-carbonyl amino acid derivatives inhibited FIH-1 based on correlations among the docking score of the FIH-1 active site, the chemical structure of the compounds, and biological HIF-α/HRE transcriptional activity.
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Penulis ;Shin-ichi Kawaguchi;Yuhei Gonda;Takuya Yamamoto;Yuki Sato;Hiroyuki Shinohara;Yohsuke Kobiki;Atsuhiko Ichimura;Takashi Dan;Motohiro Sonoda;Toshio Miyata;Akiya Ogawa;Tadayuki Tsujita
Jurnal Journal of ethnopharmacology
Tahun 2018
DOI
10.3390/molecules23040885
URL
http://www.mdpi.com/1420-3049/23/4/885
Kata Kunci
furan hypoxia inducible factor factor inhibiting hypoxia inducible factor

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