Academic Journal
Rhodacyanine derivative selectively targets cancer cells and overcomes tamoxifen resistance.
| العنوان: | Rhodacyanine derivative selectively targets cancer cells and overcomes tamoxifen resistance. |
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| المؤلفون: | John Koren, Yoshinari Miyata, Janine Kiray, John C O'Leary, Lana Nguyen, Jianping Guo, Laura J Blair, Xiaokai Li, Umesh K Jinwal, Jin Q Cheng, Jason E Gestwicki, Chad A Dickey |
| المصدر: | PLoS ONE, Vol 7, Iss 4, p e35566 (2012) |
| بيانات النشر: | Public Library of Science (PLoS) |
| سنة النشر: | 2012 |
| المجموعة: | Directory of Open Access Journals: DOAJ Articles |
| مصطلحات موضوعية: | Medicine, Science |
| الوصف: | 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. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| تدمد: | 1932-6203 |
| Relation: | http://europepmc.org/articles/PMC3338522?pdf=render; https://doaj.org/toc/1932-6203; https://doaj.org/article/5a1f2f7e12414802a13741110362ebfe |
| DOI: | 10.1371/journal.pone.0035566 |
| الاتاحة: | https://doi.org/10.1371/journal.pone.0035566 https://doaj.org/article/5a1f2f7e12414802a13741110362ebfe |
| رقم الانضمام: | edsbas.1399C057 |
| قاعدة البيانات: | BASE |
Full Text Finder | تدمد: | 19326203 |
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| DOI: | 10.1371/journal.pone.0035566 |