Preferential induction of G1 arrest in androgen-responsive human prostate cancer cells by androgen receptor signaling antagonists DL3 and antiandrogen bicalutamide
- Resource Type
- Article
- Authors
- Lu, Shan; Tan, Zongqin; Wortman, Matthew; Dong, Zhongyun
- Source
- Cancer Letters. Dec2010, Vol. 298 Issue 2, p250-257. 8p.
- Subject
- *ANTIANDROGENS
*PROSTATE cancer
*CELL receptors
*CELL cycle
*FLUORESCENCE
*PYRIMIDINES
*ANTIGENS
- Language
- ISSN
- 0304-3835
Abstract: The purpose of this study was to further characterize cell growth-inhibitory effects of a recently identified androgen receptor (AR) signaling inhibitor 6-amino-2-[2-(4-tert-butyl-pnenoxy)-ethylsulfanyl]-1H-pyrimidin-4-one (DL3)5 and antiandrogen bicalutamide (Bic). DL3 was more potent than Bic in induction of G1 arrest and reduction of G1-related cell cycle protein expression in AR-positive LNCaP cells. DL3, but not Bic, moderately inhibited growth of AR-negative PC-3 cells independent of G1 arrest. The data indicated that DL3 inhibit cell growth in both AR-dependent and -independent manners and is potentially a potent therapeutic agent for the management of advanced human prostate cancer. [ABSTRACT FROM AUTHOR]