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Gene expression analysis of HCT116 colon tumor-derived cells treated with the polyamine analog PG-11047
Natalia A Ignatenko1, Hagit F Yerushalmi, Ritu Pandey
1Department of Cell Biology and Anatomy, Arizona Cancer Center, The University of Arizona, Tucson, AZ 85724, USA. nignatenko@azcc.arizona.edu
Background:
The conformationally restricted polyamine analog PG-11047 has significant growth inhibitory activity against prostate and lung cancer cell lines and is currently under evaluation in several clinical trials, both alone and in combination with other drugs, for the treatment of relapsed or refractory cancer. The objective of this study was to identify the molecular signature of genes responsive to PG-11047 treatment and the biochemical effects of this drug in the HCT116 colon cancer cell line.
Materials And Methods:
Gene expression analysis was performed using Affymetrix GeneChip human genome U133 Plus 2.0 arrays. Changes in protein expression were evaluated using 2D polyacrylamide gels followed by LCMS/MS.
Results:
Treatment of cells with PG-11047 at concentrations ranging from 0.1 to 10 microM caused inhibition of cell growth. The activity of PG-11047 was found to correlate with its transcriptional effects on cell cycle control, focal adhesion, adherent and gap junction genes, MAPK-, Wnt- and, TGF-beta signaling pathways, transport and DNA/RNA transcription factor genes. PG-11047 caused depletion of polyamine pools. Proteomics analysis showed that PG-11047 restricts the modification of eukaryotic translation initiation factor 5A (eIF5A), resulting in suppression of general protein synthesis in PG-11047-treated cells.
Conclusion:
These data show that PG-11047 has a broad spectrum of anticancer activity in colon cancer cells.
Insights
PG-11047, a polyamine analog, inhibits colon cancer cell growth by affecting cell cycle and signaling pathways. It also suppresses protein synthesis by restricting eukaryotic translation initiation factor 5A modification.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- PG-11047 is a conformationally restricted polyamine analog with demonstrated anti-cancer activity.
- It is currently in clinical trials for relapsed or refractory cancers.
Purpose of the Study:
- To determine the molecular signature of genes affected by PG-11047 in HCT116 colon cancer cells.
- To investigate the biochemical effects of PG-11047.
Main Methods:
- Gene expression profiling using Affymetrix GeneChip arrays.
- Proteomics analysis via 2D gel electrophoresis and LC-MS/MS.
Main Results:
- PG-11047 inhibited HCT116 cell growth in a dose-dependent manner.
- Transcriptional effects were observed on cell cycle, focal adhesion, and signaling pathways (MAPK, Wnt, TGF-beta).
- PG-11047 depleted polyamine pools and suppressed protein synthesis by inhibiting eIF5A modification.
Conclusions:
- PG-11047 exhibits broad-spectrum anticancer activity in colon cancer cells.
- The drug impacts multiple cellular processes, including cell cycle regulation and protein synthesis.
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