Rhodacyanine Derivative Selectively Targets Cancer Cells and Overcomes Tamoxifen Resistance

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

PLOS ONE, 2012, vol. 7, issue 4, 1-8

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.

Date: 2012
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Persistent link: https://EconPapers.repec.org/RePEc:plo:pone00:0035566

DOI: 10.1371/journal.pone.0035566

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