Journal
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
Volume 357, Issue 2, Pages 341-346Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bbrc.2007.03.116
Keywords
T0901317; antiandrogen; androgen; AR; LNCaP; PSA; LXR agonist
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Funding
- NCCIH NIH HHS [R01 AT000850, R01 AT000850-03, AT00850] Funding Source: Medline
- NCI NIH HHS [R01 CA058073, R01 CA058073-16, CA58073] Funding Source: Medline
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T0901317 is a potent non-steroidal synthetic liver X receptor (LXR) agonist. T0901317 blocked androgenic stimulation of the proliferation of androgen-dependent LNCaP 104-S cells and androgenic suppression of the proliferation of androgen-independent LNCaP 104-R2 cells, inhibited the transcriptional activation of an androgen-dependent reporter gene by androgen, and suppressed gene and protein expression of prostate specific antigen (PSA), a target gene of androgen receptor (AR) without affecting gene and protein expression of AR. T0901317 also inhibited binding of a radiolabeled androgen to AR, but inhibition was much weaker compared to the effect of the antiandrogens, bicalutamide and hydroxyflutamide. The LXR agonist T0901317, therefore, acts as an antiandrogen in human prostate cancer cells. (c) 2007 Elsevier Inc. All rights reserved.
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