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.

Molecular engineering of supramolecular scaffold coatings that can reduce static platelet adhesion.

Novel supramolecular coatings that make use of low-molecular weight ditopic monomers with guanine end groups are studied using fluid tapping AFM. These molecules assemble on highly oriented pyrolytic graphite (HOPG) from aqueous solutions to form nanosized banding structures whose sizes can be systematically tuned at the nanoscale by tailoring the molecular structure of the monomers. The nature of the self-assembly in these systems has been studied through a combination of the self-assembly of structural derivatives and molecular modeling. Furthermore, we introduce the concept of using these molecular assemblies as scaffolds to organize functional groups on the surface. As a first demonstration of this concept, scaffold monomers that contain a monomethyl triethyleneglycol branch were used to organize these "functional" units on a HOPG surface. These supramolecular grafted assemblies have been shown to be stable at biologically relevant temperatures and even have the ability to significantly reduce static platelet adhesion.