Suppression of multidrug resistance by migrastatin

Yasushi Takemoto, Etsu Tashiro, Masaya Imoto

Research output: Contribution to journalArticlepeer-review

11 Citations (Scopus)


Migrastatin (MGS) is a Streptomyces metabolite that inhibits cancer cell migration. In this study, we found that MGS also enhanced the cytotoxicity of vinblastine, vincristine, and taxol in P-glycoprotein-overexpressing VJ-300 cells and P388/VCR cells. Furthermore, MGS increased the intracellular concentration of labeled vinblastine, vincristine, and taxol in both VJ-300 cells and P388/VCR cells. P-glycoprotein was photolabeled with [ 3H]azidopine, but this photolabeling was significantly inhibited in the presence of MGS. These results indicated that MGS directly interacts with and inhibits P-glycoprotein, thereby sensitizing drug-resistant cells to anticancer drugs.

Original languageEnglish
Pages (from-to)435-438
Number of pages4
JournalJournal of Antibiotics
Issue number7
Publication statusPublished - 2006 Jul
Externally publishedYes


  • Anticancer drugs
  • Migrastatin
  • Multi drug resistance
  • P-glycoprotein

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


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