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

5 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

Fingerprint

Polymerization
Actins
Molecules
Actin Cytoskeleton
clavilactone B
Assays
Screening
Phenotype

Keywords

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

ASJC Scopus subject areas

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

Cite this

Miyazaki, S., Sasazawa, Y., Mogi, T., Suzuki, T., Yoshida, K., Dohmae, N., ... Simizu, S. (2016). Identification of seco-clavilactone B as a small-molecule actin polymerization inhibitor. FEBS Letters, 590(8), 1163-1173. https://doi.org/10.1002/1873-3468.12154

Identification of seco-clavilactone B as a small-molecule actin polymerization inhibitor. / Miyazaki, So; Sasazawa, Yukiko; Mogi, Takuma; Suzuki, Takehiro; Yoshida, Keisuke; Dohmae, Naoshi; Takao, Kenichi; Simizu, Siro.

In: FEBS Letters, Vol. 590, No. 8, 01.04.2016, p. 1163-1173.

Research output: Contribution to journalArticle

Miyazaki, S, Sasazawa, Y, Mogi, T, Suzuki, T, Yoshida, K, Dohmae, N, Takao, K & Simizu, S 2016, 'Identification of seco-clavilactone B as a small-molecule actin polymerization inhibitor', FEBS Letters, vol. 590, no. 8, pp. 1163-1173. https://doi.org/10.1002/1873-3468.12154
Miyazaki S, Sasazawa Y, Mogi T, Suzuki T, Yoshida K, Dohmae N et al. Identification of seco-clavilactone B as a small-molecule actin polymerization inhibitor. FEBS Letters. 2016 Apr 1;590(8):1163-1173. https://doi.org/10.1002/1873-3468.12154
Miyazaki, So ; Sasazawa, Yukiko ; Mogi, Takuma ; Suzuki, Takehiro ; Yoshida, Keisuke ; Dohmae, Naoshi ; Takao, Kenichi ; Simizu, Siro. / Identification of seco-clavilactone B as a small-molecule actin polymerization inhibitor. In: FEBS Letters. 2016 ; Vol. 590, No. 8. pp. 1163-1173.
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