BPR1K653, a Novel Aurora Kinase Inhibitor, Exhibits Potent Anti-Proliferative Activity in MDR1 (P-gp170)-Mediated Multidrug-Resistant Cancer Cells
2011

BPR1K653: A New Drug for Cancer Treatment

Sample size: 11 publication 10 minutes Evidence: high

Author Information

Author(s): Cheung Chun Hei Antonio, Lin Wen-Hsing, Hsu John Tsu-An, Hour Tzyh-Chyuan, Yeh Teng-Kuang, Ko Shengkai, Lien Tzu-Wen, Coumar Mohane Selvaraj, Liu Jin-Fen, Lai Wen-Yang, Shiao Hui-Yi, Lee Tian-Ren, Hsieh Hsing-Pang, Chang Jang-Yang

Primary Institution: National Institute of Cancer Research, National Health Research Institutes, Tainan, Taiwan R.O.C.

Hypothesis

Can BPR1K653 effectively inhibit cancer cell growth regardless of MDR1 expression?

Conclusion

BPR1K653 is a potent anti-cancer compound that works effectively against both drug-sensitive and drug-resistant cancer cells.

Supporting Evidence

  • BPR1K653 inhibited Aurora-A and Aurora-B kinase activity at low concentrations.
  • It showed potent anti-proliferative activity against various cancer cell lines.
  • BPR1K653 induced apoptosis in both MDR1-negative and MDR1-positive cancer cells.
  • It effectively reduced tumor growth in xenograft models.
  • BPR1K653's effectiveness was not affected by MDR1 expression.
  • It exhibited favorable pharmacokinetic properties in rats.
  • BPR1K653 was well-tolerated with minimal toxicity in animal models.

Takeaway

BPR1K653 is a new medicine that helps fight cancer, even in cases where other treatments don't work.

Methodology

The study involved in vitro and in vivo experiments to assess the effectiveness of BPR1K653 on various cancer cell lines and xenograft models.

Statistical Information

P-Value

p<0.05

Statistical Significance

p<0.05

Digital Object Identifier (DOI)

10.1371/journal.pone.0023485

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