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Characterization of next‐generation anti‐androgens as potential prostate cancer therapeutics
Author(s) -
Jobbagy Soma,
Sikes Robert Allen,
Koh John Tzetzun
Publication year - 2011
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.25.1_supplement.968.2
Subject(s) - lncap , prostate cancer , androgen receptor , cancer research , androgen , prostate , medicine , cancer , chemistry , endocrinology , oncology , hormone
Anti‐androgens are the gold standard of care for treatment of advanced prostate cancer (PCa). The purpose of this study was to characterize novel anti‐androgens PLM1, PLM6, and PAN52 designed and synthesized in the Koh laboratory. PLM6 and PAN52 but not PLM1 are thought to have unique mechanisms of action based on their ability to evade progression to anti‐androgen resistance in vitro. Western blot analysis of nuclear fractions showed correlation between prevention of AR nuclear translocation and progression of anti‐androgen resistance in prostate cancer cell lines. Some differences in localization effects were also observed between LNCaP and CWR22Rv1 PCa models that may reflect AR mutants present in these cell lines. The compound PLM6 and PAN52 found to down‐regulate the androgen receptor (AR) in PCa cell lines. These compounds thus appear to hold promise as therapy for advanced prostate cancer. This work funded by the Beckman Foundation and the National Institutes of Health 5R01DK054257