P-glycoprotein-mediated transcellular transport of MDR-reversing agents

Tohru Saeki, Kazumitsu Ueda, Yusuke Tanigawara, Ryohei Hori, Tohru Komano

Research output: Contribution to journalArticlepeer-review

91 Citations (Scopus)


Understanding of the interactions between P-glycoprotein and multidrug resistance (MDR) reversing agents is important in designing more effective MDR modulators. We examined transcellular transport of several MDR modulators by using a drug-sensitive epithelial cell line, LLC-PK1 and its transformant cell line, LLC-GA5-COL300, which expresses human P-glycoprotein on the apical surface. Basal-to-apical transports of azidopine and diltiazem across the LLC-GA5-COL300 monolayer were increased and apical-to-basal transports were decreased compared to those across the LLC-PK1 monolayer, indicating that P-glycoprotein transports azidopine and diltiazem. Movements of nitrendipine and staurosporine across the epithelial monolayer were not affected by P-glycoprotein. These results suggests that some MDR modulators exert their inhibitory effect not only by blocking the initial binding of anticancer drugs but throughout the course of the transport process.

Original languageEnglish
Pages (from-to)99-102
Number of pages4
JournalFEBS Letters
Issue number1
Publication statusPublished - 1993 Jun 7
Externally publishedYes


  • LLC-PK
  • MDR modulator
  • Multidrug resistance
  • P-glycoprotein
  • Transcellular transport

ASJC Scopus subject areas

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


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