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Cancer Accumulation and Anticancer Activity of "CROX (Cluster Regulation of RUNX)" PIP in HER2-Positive Gastric
Tatsuya Masuda1,2, Takayoshi Watanabe1, Yasutoshi Tatsumi1
1Division of Molecular Carcinogenesis, Chiba Cancer Center Research Institute, Chiba, Japan.
Background:
We have focused on pyrrole-imidazole (PI) polyamide compounds, which preferentially bind to their target DNA sequences. To validate our "CROX (Cluster Regulation of RUNX)" strategy, we have created a novel PI polyamide-based inhibitor against RUNX termed Chb-M'. Recently, we have confirmed its cancer-specific uptake in mouse xenograft derived from HER2-positive gastric cancer cells. The accumulation and efficacy of Chb-M' in cancer has not yet been investigated in vivo, which is a simpler and less expensive method other than mouse xenograft models.
Methods:
In the present study, we have employed the simple and versatile experimental system termed CAM (chorioallantoic membrane) model, and evaluated whether Chb-M' could have the cancer accumulation potential and anti-cancer activity.
Results:
Based on our present results, gastric cancer MKN45 cells transplanted onto CAM successfully developed cancers, and the intravenously injected FITC-labeled Chb-M' obviously accumulated in these CAM cancers. As expected, the treatment of the CAM cancers with Chb-M' significantly attenuated the growth of the CAM cancers. Our present results were basically identical to those obtained from mouse xenograft model.
Conclusion:
Our present findings strongly suggest that Chb-M' preferentially accumulates in cancer to suppress its growth, and the CAM model might serve as a valuable and promising platform to rapidly assess the cancer uptake and anti-cancer efficacy of various PI polyamide-based drug candidates.
Insights
Pyrrole-imidazole (PI) polyamides like Chb-M' show cancer-specific uptake and inhibit tumor growth. The chorioallantoic membrane (CAM) model effectively evaluates PI polyamide efficacy and accumulation in vivo.
Area of Science:
- Medicinal Chemistry
- Oncology
- Molecular Biology
Background:
- Pyrrole-imidazole (PI) polyamides are designed for targeted DNA binding.
- A novel PI polyamide, Chb-M', was developed as a RUNX inhibitor.
- Previous studies confirmed Chb-M' cancer-specific uptake in HER2-positive gastric cancer xenografts.
Purpose of the Study:
- To validate the "CROX (Cluster Regulation of RUNX)" strategy using Chb-M'.
- To investigate the in vivo accumulation and anti-cancer efficacy of Chb-M' using a simpler model than mouse xenografts.
Main Methods:
- Utilized the chorioallantoic membrane (CAM) model for in vivo evaluation.
- Assessed cancer accumulation potential and anti-cancer activity of Chb-M' in CAM models.
Main Results:
- Gastric cancer cells (MKN45) successfully developed on CAM.
- FITC-labeled Chb-M' demonstrated significant accumulation in CAM cancers.
- Chb-M' treatment significantly inhibited the growth of CAM cancers, mirroring results from mouse xenografts.
Conclusions:
- Chb-M' preferentially accumulates in cancer and suppresses its growth.
- The CAM model serves as a valuable platform for rapid assessment of PI polyamide drug candidates.
- Findings support the potential of PI polyamides in cancer therapy.
