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Rhodacyanine derivative selectively targets cancer cells and overcomes tamoxifen resistance.

  • Author(s): Koren, John
  • Miyata, Yoshinari
  • Kiray, Janine
  • O'Leary, John C
  • Nguyen, Lana
  • Guo, Jianping
  • Blair, Laura J
  • Li, Xiaokai
  • Jinwal, Umesh K
  • Cheng, Jin Q
  • Gestwicki, Jason E
  • Dickey, Chad A
  • et al.

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.

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