Comparative proteomic analysis reveals growth inhibition by 3-N-alkyloxyestradiol derivative (SERM) in prostate cancer cells.

Background/aim: In this study we evaluated the proteomic profile of PC-3 cells treated with novel, 3-N-alkyloxyestradiol derivative, 3-[2-diisopropylamino]-ethoxy-D1,3,5 (10)-estrien-17-one (DI) (USPTO #7,687,486).

Materials And Methods: The growth inhibitory potential of DI was determined by the National Cancer Institute (NCI) Developmental Therapeutics Program. 2-D gel electrophoresis and mass spectrometry were employed to identify differentially expressed proteins after treatment with DI.

Results: Growth inhibitory (GI(50)) results showed that DI inhibited the growth of PC-3 and DU-145 cells, at 13.9 μM and 30.8 μM, respectively. Out of the proteins differentially expressed, five were selected for identification with four of those being successfully identified. The identified proteins play a role in protein folding, cell motility, carbohydrate biosynthesis, and carbohydrate degradation.

Conclusion: Our studies resulted in the identification of targets associated with the glycolytic pathway and cell motility which have been implicated in the development and progression of many cancers.