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Title: The liver X receptor agonist T0901317 acts as androgen receptor antagonist in human prostate cancer cells

Abstract

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.

Authors:
 [1];  [2];  [1];  [1];  [1];  [2];  [3]
  1. The Ben May Department for Cancer Research, The University of Chicago, CIS W325F, 929 E. 57th Street, Chicago, IL 60637 (United States)
  2. Department of Biological, Chemical, and Physical Science, Illinois Institute of Technology, 3101 South Dearborn Street, Chicago, IL 60616 (United States)
  3. The Ben May Department for Cancer Research, The University of Chicago, CIS W325F, 929 E. 57th Street, Chicago, IL 60637 (United States). E-mail: sliao@uchicago.edu
Publication Date:
OSTI Identifier:
20991360
Resource Type:
Journal Article
Resource Relation:
Journal Name: Biochemical and Biophysical Research Communications; Journal Volume: 357; Journal Issue: 2; Other Information: DOI: 10.1016/j.bbrc.2007.03.116; PII: S0006-291X(07)00553-0; Copyright (c) 2007 Elsevier Science B.V., Amsterdam, The Netherlands, All rights reserved; Country of input: International Atomic Energy Agency (IAEA)
Country of Publication:
United States
Language:
English
Subject:
62 RADIOLOGY AND NUCLEAR MEDICINE; ANDROGENS; ANTIANDROGENS; ANTIGENS; CARCINOMAS; CELL PROLIFERATION; GENES; INHIBITION; LIVER; PROSTATE; RECEPTORS; STIMULATION

Citation Formats

Chuu, Chih-pin, Chen, Rou-Yu, Hiipakka, Richard A., Kokontis, John M., Warner, Karen V., Xiang, Jialing, and Liao, Shutsung. The liver X receptor agonist T0901317 acts as androgen receptor antagonist in human prostate cancer cells. United States: N. p., 2007. Web. doi:10.1016/j.bbrc.2007.03.116.
Chuu, Chih-pin, Chen, Rou-Yu, Hiipakka, Richard A., Kokontis, John M., Warner, Karen V., Xiang, Jialing, & Liao, Shutsung. The liver X receptor agonist T0901317 acts as androgen receptor antagonist in human prostate cancer cells. United States. doi:10.1016/j.bbrc.2007.03.116.
Chuu, Chih-pin, Chen, Rou-Yu, Hiipakka, Richard A., Kokontis, John M., Warner, Karen V., Xiang, Jialing, and Liao, Shutsung. Fri . "The liver X receptor agonist T0901317 acts as androgen receptor antagonist in human prostate cancer cells". United States. doi:10.1016/j.bbrc.2007.03.116.
@article{osti_20991360,
title = {The liver X receptor agonist T0901317 acts as androgen receptor antagonist in human prostate cancer cells},
author = {Chuu, Chih-pin and Chen, Rou-Yu and Hiipakka, Richard A. and Kokontis, John M. and Warner, Karen V. and Xiang, Jialing and Liao, Shutsung},
abstractNote = {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.},
doi = {10.1016/j.bbrc.2007.03.116},
journal = {Biochemical and Biophysical Research Communications},
number = 2,
volume = 357,
place = {United States},
year = {Fri Jun 01 00:00:00 EDT 2007},
month = {Fri Jun 01 00:00:00 EDT 2007}
}