Inhibition of neuraminidase by Ganoderma triterpenoids and implications for neuraminidase inhibitor design

Qinchang Zhu, Tran Hai Bang, Koichiro Ohnuki, Takashi Sawai, Ken Sawai, Kuniyoshi Shimizu

研究成果: Contribution to journalArticle査読

29 被引用数 (Scopus)

抄録

Neuraminidase (NA) inhibitors are the dominant antiviral drugs for treating influenza in the clinic. Increasing prevalence of drug resistance makes the discovery of new NA inhibitors a high priority. Thirty-one triterpenoids from the medicinal mushroom Ganoderma lingzhi were analyzed in an in vitro NA inhibition assay, leading to the discovery of ganoderic acid T-Q and TR as two inhibitors of H5N1 and H1N1 NAs. Structure-activity relationship studies revealed that the corresponding triterpenoid structure is a potential scaffold for the design of NA inhibitors. Using these triterpenoids as probes we found, through further in silico docking and interaction analysis, that interactions with the amino-acid residues Arg292 and/or Glu119 of NA are critical for the inhibition of H5N1 and H1N1. These findings should prove valuable for the design and development of NA inhibitors.

本文言語英語
論文番号13194
ジャーナルScientific reports
5
DOI
出版ステータス出版済み - 8 26 2015

All Science Journal Classification (ASJC) codes

  • General

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