Prostate cancer: Antiandrogens reverse docetaxel resistance via ABCB1 inhibition

@article{Fenner2015ProstateCA,
  title={Prostate cancer: Antiandrogens reverse docetaxel resistance via ABCB1 inhibition},
  author={Annette Fenner},
  journal={Nature Reviews Urology},
  year={2015},
  volume={12},
  pages={361-361}
}
Antiandrogens such as bicalutamide and enzalutamide can resensitize docetaxelresistant prostate cancer cells to docetaxel treatment, by inhibiting efflux of the ATP-binding cassette (ABC) transporter ABCB1, according to a study published in Clinical Cancer Research. ABC transporters carry substances, including docetaxel, out of cells, reducing their intracellular concentration and, therefore, their efficacy. ABCB1 overexpression has been shown to confer resistance to chemotherapy and is… Expand
1 Citations
Targeting TR4 nuclear receptor with antagonist bexarotene increases docetaxel sensitivity to better suppress the metastatic castration-resistant prostate cancer progression
TLDR
It is suggested that targeting this newly identified TR4/lincRNA-p21/HIF-1α/VEGF-A signaling with Bex, an FDA-approved drug, may increase the DTX chemo-sensitivity to better suppress the mCRPC progression. Expand

References

Antiandrogens Inhibit ABCB1 Efflux and ATPase Activity and Reverse Docetaxel Resistance in Advanced Prostate Cancer
TLDR
A novel mechanism of action for antiandrogens such as bicalutamide and enzalutamide as inhibitors of ABCB1 efflux and ATPase activity is identified and may lead to the development of combinational therapies to treat advanced prostate cancer independent of AR status, and possibly other types of cancer. Expand