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Identification of a Raloxifene Analog That Promotes AhR-Mediated Apoptosis in Cancer Cells by Hyo Jang; Martin Pearce; Edmond O’Donnell; Bach Nguyen; Lisa Truong; Monica Mueller; William Bisson; Nancy Kerkvliet; Robert Tanguay; Siva Kolluri is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Identification of a Raloxifene Analog That Promotes AhR-Mediated Apoptosis in Cancer Cells about?
We previously reported that raloxifene, an estrogen receptor modulator, is also a ligand for the aryl hydrocarbon receptor (AhR). Raloxifene induces apoptosis in estrogen receptor-negative human cancer cells through the AhR. We performed structure-activity studies with seven raloxifene analogs to better understand the structural requirements of raloxifene for induction of AhR-mediated transcriptional activity and apoptosis. We identified Y134 as a raloxifene analog that activates AhR-mediated transcriptional activity and induces apoptosis in MDA-MB-231 human triple negative breast cancer cells. Suppression of AhR expression strongly reduced apoptosis induced by Y134, indicating the requirement of AhR for Y134-induced apoptosis. Y134 also induced apoptosis in hepatoma cells without having an effect on cell cycle regulation. Toxicity testing on zebrafish embryos revealed that Y134 has a significantly better safety profile than raloxifene. Our studies also identified an analog of raloxifene that acts as a partial antagonist of the AhR, and is capable of inhibiting AhR agonist-induced transcriptional activity. We conclude that Y134 is a promising raloxifene analog for further optimizat
Who reads Identification of a Raloxifene Analog That Promotes AhR-Mediated Apoptosis in Cancer Cells?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Hyo Jang; Martin Pearce; Edmond O’Donnell; Bach Nguyen; Lisa Truong; Monica Mueller; William Bisson; Nancy Kerkvliet; Robert Tanguay; Siva Kolluri
- Publisher
- MDPI AG
- Published
- 2017
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)