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Rhodacyanine Derivative Selectively Targets Cancer Cells and Overcomes Tamoxifen Resistance

Author

Listed:
  • John Koren III
  • Yoshinari Miyata
  • Janine Kiray
  • John C O'Leary III
  • Lana Nguyen
  • Jianping Guo
  • Laura J Blair
  • Xiokai Li
  • Umesh K Jinwal
  • Jin Q Cheng
  • Jason E Gestwicki
  • Chad A Dickey

Abstract

MKT-077, a rhodacyanine dye, was shown to produce cancer specific cell death. However, complications prevented the use of this compound beyond clinical trials. Here we describe YM-1, a derivative of MKT-077. We found that YM-1 was more cytotoxic and localized differently than MKT-077. YM-1 demonstrated this cytotoxicity across multiple cancer cell lines. This toxicity was limited to cancer cell lines; immortalized cell models were unaffected. Brief applications of YM-1 were found to be non-toxic. Brief treatment with YM-1 restored tamoxifen sensitivity to a refractory tamoxifen-resistant MCF7 cell model. This effect is potentially due to altered estrogen receptor alpha phosphorylation, an outcome precipitated by selective reductions in Akt levels (Akt/PKB). Thus, modifications to the rhodocyanine scaffold could potentially be made to improve efficacy and pharmacokinetic properties. Moreover, the impact on tamoxifen sensitivity could be a new utility for this compound family.

Suggested Citation

  • John Koren III & Yoshinari Miyata & Janine Kiray & John C O'Leary III & Lana Nguyen & Jianping Guo & Laura J Blair & Xiokai Li & Umesh K Jinwal & Jin Q Cheng & Jason E Gestwicki & Chad A Dickey, 2012. "Rhodacyanine Derivative Selectively Targets Cancer Cells and Overcomes Tamoxifen Resistance," PLOS ONE, Public Library of Science, vol. 7(4), pages 1-8, April.
    • Handle: RePEc:plo:pone00:0035566
    DOI: 10.1371/journal.pone.0035566
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