RV59 is a small molecule, a derivative of EGFR inhibitor osimertinib derivative [41,42], which was recently synthesized in our laboratory. The anticancer effects of the RV59 was evaluated using the US National Cancer Institute (NCI)-60 colon cancer cells to single-dose and dose-dependent treatments with RV59 .

RV59 kills cNrf2-mediated 5-FU resistance in colon cancer cells via apoptotic pathway. A. The IC50 value of RV-59 for p53-/-HCT116 cells, NLS-mutated Nrf2-transfected shNrf2-HCT116 stable clones and normal FHC colon epithelial cells was calculated from their dose response survival curves. Each cells were treated with RV-59 for 48 h. B.

RV-59 suppresses cytoplasmic Nrf2-mediated 5-fluorouracil resistance and tumor growth in colorectal cancer. Ching-Ju Shen1, Po-Lin Lin2, Hsiao-Ching Lin2, Ya-Wen Cheng3,4, Hsu-Shan Huang , Huei Lee2.

Moreover, we compared results obtained from RV59 docking with standard inhibitors of MYC (vorinostat), CXCL8 (reparixin), and TIMP1 (ilomastat). ... ... free binding energy results were obtained...

Aug 1, 2021 · RV-59 suppresses cytoplasmic Nrf2-mediated 5-fluorouracil resistance and tumor growth in colorectal cancer. The results strongly suggest that RV-59 may be a novel antitumor agent for suppression of 5-FU resistance and may have therapeutic potential for improving outcomes in patients with cNrf2-expressing tumors.

RV59 displayed anti-proliferative and cytotoxic effects in NC-I60 human colon cancer cell lines. (A) A singledose treatment administered at 10 μM, revealed growth percentage cytotoxic effects of...

Dec 1, 2019 · These results strongly suggest that RV-59 may be a novel antitumor agent for suppression of 5-FU resistance and may have therapeutic potential for improving outcomes in patients with cNrf2-expressing tumors. Keywords: 5-fluorouracil; Nrf2; and colorectal cancer.

The results strongly suggest that RV-59 may be a novel antitumor agent for suppression of 5-FU resistance and may have therapeutic potential for improving outcomes in patients with cNrf2-expressing tumors. Our previous studies indicated that tumor invasion and 5-flurouracil (5-FU) resistance in colorectal cancer (CRC) was more affected by cytoplasmic localization of expressed Nrf2 (cNrf2) than ...

Our previous studies indicated that tumor invasion and 5-flurouracil (5-FU) resistance in colorectal cancer (CRC) was more affected by cytoplasmic localization of expressed Nrf2 (cNrf2) than by nuclear localization (nNrf2), indicating a need for novel antitumor agents to overcome 5-FU resistance and improve outcomes in patients with CRC. In the present study, 20 nitrogen-substituted anthra[1,2 ...

Dec 1, 2019 · PDF | Our previous studies indicated that tumor invasion and 5-flurouracil (5-FU) resistance in colorectal cancer (CRC) was more affected by cytoplasmic... | Find, read and cite all the research ...