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Identification of seco‐clavilactone B as a small‐molecule actin polymerization inhibitor
Author(s) -
Miyazaki So,
Sasazawa Yukiko,
Mogi Takuma,
Suzuki Takehiro,
Yoshida Keisuke,
Dohmae Naoshi,
Takao Kenichi,
Simizu Siro
Publication year - 2016
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1002/1873-3468.12154
Subject(s) - actin , polymerization , chemistry , actin binding protein , protein filament , in vitro , actin remodeling , mdia1 , biochemistry , microfilament , actin cytoskeleton , cytoskeleton , cell , polymer , organic chemistry
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.