Non-competitive androgen receptor inhibition in vitro and in vivo
@article{Jones2009NoncompetitiveAR, title={Non-competitive androgen receptor inhibition in vitro and in vivo}, author={J. O. Jones and Eric C Bolton and Y. Huang and Cl{\'e}mentine F{\'e}au and R. Guy and K. Yamamoto and B. Hann and M. Diamond}, journal={Proceedings of the National Academy of Sciences}, year={2009}, volume={106}, pages={7233 - 7238} }
Androgen receptor (AR) inhibitors are used to treat multiple human diseases, including hirsutism, benign prostatic hypertrophy, and prostate cancer, but all available anti-androgens target only ligand binding, either by reduction of available hormone or by competitive antagonism. New strategies are needed, and could have an important impact on therapy. One approach could be to target other cellular mechanisms required for receptor activation. In prior work, we used a cell-based assay of AR… Expand
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References
SHOWING 1-10 OF 32 REFERENCES
A cellular conformation-based screen for androgen receptor inhibitors.
- Biology, Medicine
- ACS chemical biology
- 2008
- 36
Activity of androgen receptor antagonist bicalutamide in prostate cancer cells is independent of NCoR and SMRT corepressors.
- Biology, Medicine
- Cancer research
- 2007
- 86
- PDF
Biology of progressive, castration-resistant prostate cancer: directed therapies targeting the androgen-receptor signaling axis.
- Medicine
- Journal of clinical oncology : official journal of the American Society of Clinical Oncology
- 2005
- 926
Molecular determinants of resistance to antiandrogen therapy
- Biology, Medicine
- Nature Medicine
- 2004
- 2,148
- Highly Influential
Cell- and gene-specific regulation of primary target genes by the androgen receptor.
- Biology, Medicine
- Genes & development
- 2007
- 316
- PDF
Molecular biology of the androgen receptor.
- Biology, Medicine
- Journal of clinical oncology : official journal of the American Society of Clinical Oncology
- 2002
- 864
Linking ligand-induced alterations in androgen receptor structure to differential gene expression: a first step in the rational design of selective androgen receptor modulators.
- Biology, Medicine
- Molecular endocrinology
- 2006
- 66
- PDF
The androgen receptor: a mediator of diverse responses.
- Biology, Medicine
- Frontiers in bioscience : a journal and virtual library
- 1996
- 100
- PDF
Mechanism of antiandrogen action: key role of hsp90 in conformational change and transcriptional activity of the androgen receptor.
- Chemistry, Medicine
- Biochemistry
- 2002
- 155