論文 - 詳細
| RRC ID | 85653 |
|---|---|
| 著者 | Masuda T, Watanabe T, Tatsumi Y, Lin J, Okumura K, Ozaki T, Sugiyama H, Kamikubo Y. |
| タイトル | Cancer Accumulation and Anticancer Activity of "CROX (Cluster Regulation of RUNX)" PIP in HER2-Positive Gastric Cancer Evaluated by Chicken Egg Cancer Model. |
| ジャーナル | Cancer Med |
| Abstract |
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. |
| 巻・号 | 14(7) |
| ページ | e70845 |
| 公開日 | 2025-4-1 |
| DOI | 10.1002/cam4.70845 |
| PMID | 40171874 |
| PMC | PMC11962651 |
| MeSH | Animals Antineoplastic Agents* / pharmacology Cell Line, Tumor Cell Proliferation / drug effects Chickens Disease Models, Animal Humans Imidazoles* / chemistry Imidazoles* / pharmacology Mice Nylons* / chemistry Nylons* / pharmacology Pyrroles* / chemistry Pyrroles* / pharmacology Receptor, ErbB-2* / metabolism Stomach Neoplasms* / drug therapy Stomach Neoplasms* / genetics Stomach Neoplasms* / metabolism Stomach Neoplasms* / pathology Xenograft Model Antitumor Assays |
| IF | 3.491 |
| リソース情報 | |
| 遺伝子材料 | CS-RfA-ETV (RDB08020) |