By a News Reporter-Staff News Editor at Drug Week -- New research on Prostate Cancer is the subject of a report. According to news reporting out of Urbana, Illinois, by NewsRx editors, research stated, "The androgen receptor (AR) has a critical role in the growth and progression of androgen-dependent and castration-resistant prostate cancers. To identify novel inhibitors of AR transactivation that block growth of prostate cancer cells, a luciferase-based high-throughput screen of ~160,000 small molecules was performed in cells stably expressing AR and a prostate-specific antigen (PSA)-luciferase reporter."
Our news journalists obtained a quote from the research, "CPIC (1-(3-(2-chlorophenoxy) propyl)-1H-indole-3-carbonitrile) was identified as a small molecule that blocks AR transactivation to a greater extent than other steroid receptors. CPIC inhibited AR-mediated proliferation of androgen-sensitive prostate cancer cell lines, with minimal toxicity in AR-negative cell lines. CPIC treatment also reduced the anchorage-independent growth of LAPC-4 prostate cancer cells. CPIC functioned as a pure antagonist by inhibiting the expression of AR-regulated genes in LAPC-4 cells that express wild-type AR and exhibited weak agonist activity in LNCaP cells that express the mutant AR-T877A. CPIC treatment did not reduce AR levels or alter its nuclear localization. We used chromatin immunoprecipitation to identify the site of action of CPIC. CPIC inhibited recruitment of androgen-bound AR to the PSA promoter and enhancer sites to a greater extent than bicalutamide."
According to the news editors, the research concluded: "CPIC is a new therapeutic inhibitor that targets AR-mediated gene activation with potential to arrest the growth of prostate cancer."
For more information on this research see: A competitive inhibitor that reduces recruitment of androgen receptor to androgen-responsive genes. Journal of Biological Chemistry, 2012;287(28):23368-80. (American Society for Biochemistry and Molecular Biology - www.asbmb.org; Journal of Biological Chemistry - www.jbc.org/)
Our news journalists report that additional information may be obtained by contacting M.T. Cherian, Dept. of BiochemistryUniversity of Illinois, Urbana, Illinois 61801-3602, United States (see also Prostate Cancer).
Keywords for this news article include: Urbana, Illinois, Genetics, Hormones, Oncology, United States, Prostate Cancer, Steroid Receptors, Androgen Receptors, Prostatic Neoplasms, DNA Binding Proteins, Transcription Factors, North and Central America, Androgens and Anabolic Steroids.
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