High YEATS2 expression activates Wnt/β-catenin signaling to promote EMT in GC and is correlated with poor prognosis of GC patients.

KDM1A regulates CRC progression by modulating epithelial-mesenchymal transition (EMT), metabolism, and Wnt signaling. Targeting KDM1A with GSK2879552 represents a promising therapeutic strategy for CRC treatment.

Importantly, treatment with XAV-939, a specific Wnt/β-catenin pathway inhibitor, abrogated the pro-oncogenic effects of SAMD4B overexpression, including Wnt/β-catenin pathway activation, enhanced proliferation, and increased metastatic capacity...In summary, our findings clarify that SAMD4B exerts an oncogenic role in breast cancer progression by activating the Wnt/β-catenin pathway. These data identify SAMD4B as a potential therapeutic target in breast cancer, although further in vivo investigations are required to validate its clinical relevance.

Pharmacological interventions using Wnt3a (activation) and XAV939 (inhibition) modulated Wnt/β-catenin signaling, while CRISPR/Cas9-mediated RelB knockout and plasmid-based overexpression established isogenic cell models...This plant-derived alkaloid exerts anti-HCC effects through Wnt pathway modulation, while compensatory RelB activation constrains therapeutic outcomes. Strategic RelB co-targeting establishes a dual pathway phytotherapy paradigm, synergistically merging botanical pharmacodynamics with precision oncology.

Additionally, a machine learning model trained on 236 known Tankyrase inhibitors accurately predicted pIC₅₀ values, with compound 138594346 (pIC₅₀ = 7.70) closely matching the reference inhibitor (pIC₅₀ = 7.71), and 138594428 also exhibiting strong predicted activity (pIC₅₀ = 7.41). Collectively, these results highlight 138594346 and 138594428 as promising candidates for further experimental validation in the development of targeted CRC therapeutics.

Basroparib (STP1002) was shown to be a safe and well-tolerated tankyrase-selective inhibitor with preliminary anti-tumor activity warranting further investigation.

JPI-547 outperformed most PARP inhibitors, with a half-maximal inhibitory concentration approximately 10-fold lower than that of olaparib. PDAC cells reliant on Wnt signaling due to pathogenic RNF43 mutations showed increased susceptibility to JPI-547 without altering homologous recombination repair efficiency. JPI-547 disrupts the Wnt/β-catenin pathway in RNF43-mutated cells and inhibits the oncogenic YAP pathway, highlighting its multifaceted therapeutic potential in PDAC with HRD or Wnt-addiction.

Collectively, these findings underscore the effectiveness of combining machine learning and system biology to accelerate rational drug discovery. Olaparib emerges as a promising candidate for TNKS-targeted therapy, providing a strong computational foundation for experimental validation and future preclinical drug development.

Functional rescue experiments confirmed that BGN overexpression reverses the inhibitory effects of GLIS2 knockdown, while the Wnt/β-catenin inhibitor XAV-939 effectively blocks BGN's tumor-promoting effects. These findings establish the crucial role of the GLIS2-BGN-Wnt/β-catenin axis in regulating GC EMT and identify novel potential therapeutic targets for GC treatment.

P2, N=40, Recruiting, Allarity Therapeutics | Active, not recruiting --> Recruiting

Our results indicate that the DJQ decoction suppresses tumor progression by inhibiting the Wnt/β-catenin pathway, offering a promising treatment approach for MM.

Notably, we found that supplementing the mTeSR1 basal medium with XAV939, a Wnt/β-catenin pathway inhibitor, supported robust self-renewal and pluripotency maintenance of SD-iPSCs. Furthermore, using a bovine trophoblast stem cells (TSC) induction protocol, we successfully derived CDX2-positive trophoblast-like cells from SD-iPSCs. The establishment of SD-iPSCs not only offers a valuable model for studying mammalian pluripotent stem cells but also provides a versatile platform for biotechnological and translational research.