Identification of seco-clavilactone B as a small-molecule actin polymerization inhibitor

So Miyazaki, Yukiko Sasazawa, Takuma Mogi, Takehiro Suzuki, Keisuke Yoshida, Naoshi Dohmae, Kenichi Takao, Siro Simizu

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

Phenotype-based chemical screening is an attractive strategy for the identification of bioactive compounds. We searched for a compound that induces cellular morphological change and identified a novel compound that we named seco-clavilactone B (Seco-CB). Treatment with Seco-CB decreased the ratio of filament actin (F-actin) to globular actin (G-actin). An in vitro actin polymerization assay revealed that Seco-CB inhibited actin polymerization directly. Further analysis demonstrated that the inhibitory effect of Seco-CB on actin polymerization was associated with Seco-CB binding to either Thr5 or Cys285 of actin. These data indicate that Seco-CB is a novel actin polymerization inhibitor.

Original languageEnglish
Pages (from-to)1163-1173
Number of pages11
JournalFEBS Letters
Volume590
Issue number8
DOIs
Publication statusPublished - 2016 Apr 1

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Keywords

  • actin polymerization inhibitor
  • bioprobe
  • chemical biology
  • cytoskeleton
  • seco-clavilactone B

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Cell Biology
  • Genetics
  • Molecular Biology
  • Structural Biology

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