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Association details:
| Biomarker: | CTNNB1 mutation |
|---|---|
| Cancer: | Endometrial Cancer |
| Drug: | foscenvivint (PRI724) (CBP inhibitor, β-catenin inhibitor, Wnt signalling pathway inhibitor) + lorecivivint (SM04690) (Wnt signalling pathway inhibitor, pan-CLK inhibitor, DYRK1A inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Targeting Wnt/beta-catenin signaling in CTNNB1-mutant endometrial cancer
Published date:
03/19/2021
Excerpt:
We studied CTNNB1-wildtype (HEC1B, Ishikawa) and CTNNB1-mutant (HEC108, HEC265, HEC1B-S33Y, Ishikawa-S33Y) EC cell lines. In contrast, PRI724 and SM04690 indirectly inhibited beta-catenin transcriptional activity and significantly reduced cell viability in CTNNB1-mutant EC cell lines. Treatment with SM04690 reduced cell viability in all EC cell lines, but was significantly lower in HEC108, HEC265 and HEC1B-S33Y...SM04690 significantly induced apoptosis in HEC265 cells (3.98% vs. 6.91% AnnexinV/PI+, p = 0.044) and reduced TCF transcriptional activity in HEC1B-S33Y (-84%, p = 0.017) and HEC108 (-74%, p = 0.002) cells.
