β-catenin antag News - LARVOL Sigma

|||||||||| Journal: Hydrogelation of peptides and carnosic acid as regulators of adaptive immunity against postoperative recurrence of cutaneous melanoma. (Pubmed Central) - Oct 17, 2024
Consequently, it effectively suppresses postoperative recurrence of skin cutaneous melanoma (SKCM) in vivo. Collectively, the presented Supra-gel?CA not only provides an efficacious immunotherapy strategy for regulating adaptive immunity by overcoming the obstacle posed by melanoma-intrinsic ?-catenin signaling-induced absence of CTLs but also offers a clinically translatable hydrogel that revolutionizes post-surgical management of SKCM.

|||||||||| foscenvivint (PRI724) / PRISM Pharma, Ohara Pharma
AN ORAL INHIBITOR OF CBP/?-CATENIN SIGNALING, C-82, IMPROVES LIVER STEATOSIS, FUNCTION, INFLAMMATION AND FIBROSIS IN THE GAN DIET-INDUCED OBESE MOUSE MODEL OF MASH () - Oct 15, 2024 - Abstract #AASLD2024AASLD_777;
C-82 treatment improves not only MASH-like liver disorders (steatosis, function and inflammation) but also liver fibrosis. C-82, an oral inhibitor of CBP/?-catenin signaling, shows a potent therapeutic effect on MASH-related liver fibrosis and steatosis.

|||||||||| telatinib (BAY 57- 9352) / EddingPharm, Mektovi (binimetinib) / Ono Pharma, Pierre Fabre, Pfizer
Journal: Discovery of Small Molecule Inhibitors Targeting CTNNB1 (?-catenin) for Endometrial cancer: Employing 3D QSAR, Drug-Likeness Assessment, ADMET Predictions, Molecular Docking and Simulation. (Pubmed Central) - Sep 25, 2024
Through a comprehensive screening process employing in silico drug design methods, this study successfully identified five potential human anticancer drug candidates targeting the beta-catenin protein. These findings offer a foundation for further experimental validation and development towards the treatment of EC.

|||||||||| gemcitabine / Generic mfg.
HYPERTHERMIA IMPROVES GEMCITABINE SENSITIVITY OF PANCREATIC CANCER CELLS BY SUPPRESSING THE EPHRIN A4/?-CATENIN AXIS AND ACTIVATING DEOXYCYTIDINE KINASE (Science Lounge) - Jul 18, 2024 - Abstract #UEGW2024UEGW_705;
These findings offer a foundation for further experimental validation and development towards the treatment of EC. This study delineates the role of hyperthermia in enhancing GEM sensitivity of PC cells, primarily mediated through the suppression of the EFNA4/?-catenin axis and activation of dCK.

|||||||||| XAV-939 / Novartis
Journal: Aerobic exercise training engages the canonical wnt pathway to improve pulmonary function and inflammation in COPD. (Pubmed Central) - May 15, 2024
The beneficial role of exercise may be exerted through Wnt/?-catenin-PPAR? pathway.

|||||||||| gemcitabine / Generic mfg.
Journal: Hyperthermia improves gemcitabine sensitivity of pancreatic cancer cells by suppressing the EFNA4/?-catenin axis and activating dCK. (Pubmed Central) - Apr 9, 2024
Consistently, in vivo, hyperthermia augmented the therapeutic efficacy of GEM on xenograft tumors through modulation of the ephrin A4/?-catenin/dCK axis. This study delineates the role of hyperthermia in enhancing GEM sensitivity of PC cells, primarily mediated through the suppression of the EFNA4/?-catenin axis and activation of dCK.

|||||||||| foscenvivint (PRI724) / PRISM Pharma, Ohara Pharma
Journal, Tumor mutational burden, PD(L)-1 Biomarker, IO biomarker: Targeting Wnt signaling for improved glioma immunotherapy. (Pubmed Central) - Mar 11, 2024
We also observed differential gene expression and induced immune cell infiltration in tumors pretreated with ICG-001 and then treated with CAR T cells as compared with single treatment groups or when ICG-001 treatment was administered after CAR T cell therapy. We conclude that specific Wnt/CBP/?-catenin antagonism results in pleotropic changes in the glioma TME, including glioma stem cell differentiation, modulation of the stroma, and immune cell activation and recruitment, thereby suggesting a possible role for enhancing immunotherapy in glioma patients.

|||||||||| ST316 / Sapience Therap
ST316, a clinical peptide antagonist of beta-catenin, induces anti-tumor immune responses by multiple mechanisms of action (Section 4) - Mar 5, 2024 - Abstract #AACR2024AACR_8304;
P1
Second, ST316 induced CD155/PVR upregulation and T-cell activation in the presence of anti-TIGIT antibody. Collectively these results suggest a novel immune-modulatory role for ST316 in the TIME and provide rational for combination therapy with checkpoint inhibitors.

|||||||||| E7386 / Eisai, PRISM Pharma
Journal: E7386 is not a Specific CBP/?-Catenin Antagonist. (Pubmed Central) - Nov 27, 2023
Collectively these results suggest a novel immune-modulatory role for ST316 in the TIME and provide rational for combination therapy with checkpoint inhibitors. It can thus be concluded that E7386 is not a specific CBP/?-catenin antagonist.

|||||||||| foscenvivint (PRI724) / PRISM Pharma, Ohara Pharma
Journal: Differential Kat3 Coactivator Usage Regulates Brain Metabolism and Neuronal Differentiation. (Pubmed Central) - Nov 21, 2023
It can thus be concluded that E7386 is not a specific CBP/?-catenin antagonist. Rebalancing the equilibrium between CBP/?-catenin versus p300/?-catenin associated transcription, utilizing the small molecule CBP/beta-catenin antagonist ICG-001, enhances mitochondrial oxidative phosphorylation, metabolic function, and neuronal differentiation and may be able to ameliorate the cognitive decline seen in neurodegenerative disorders, including Alzheimer's Disease.

|||||||||| Actionable Findings from an Unbiased Drug Screen for Novel Single Agent and Combination Therapies Against AML with Mecom Re-Arrangement (SDCC - Halls G-H) - Nov 3, 2023 - Abstract #ASH2023ASH_1826;
This was consistent with previous reports that BET inhibitors (e.g., OTX015, mivebresib or ABBV-075 and JQ1) are effective against 3q26.2-r AML cell lines, patient-derived (PD) AML cells and PDX models...In follow-up experiments, XIAP/cIAPs inhibitors birinapant (10-1000 nM) or SM-164 (30-1000 nM), chosen based on the MIPE screen outcomes, induced significantly more dose-dependent apoptosis in 3q26.2-r versus the other AML cell lines...Treatment with the dual mTOR/PIK3CA inhibitor NVP-BGT226 (1-30 nM) or navitoclax or Bcl-xL-specific BH3 mimetic A-1155463 also exerted lethality and synergistically induced apoptosis with mivebresib in AML cells with inv3/t(3;3)...Co-treatment with birinapant and tegavivint also synergistically induced apoptosis in 3q26.2-r AML cells...Additionally, compared to each drug or vehicle control, co-treatment with birinapant and the BETi OTX015 (30 mg/kg/day, by oral gavage) was more effective in reducing AML burden in the xenograft model. These findings demonstrate promising preclinical activity of IAP protein inhibition against the cellular models of AML with inv3/t(3;3) with EVI1 overexpression, supporting the rationale to further evaluate in vivo efficacy of birinapant and/or BETi-based combinations against this AML sub-type.

|||||||||| Preclinical, Journal: A Mouse Model for the Rapid and Binomial Assessment of Putative WNT/?-Catenin Signalling Inhibitors. (Pubmed Central) - Oct 28, 2023
Indeed, the phenotypic plasticity of born Apc conceptus enables future refinement of our assay to potentially enable dosage finding and cross-compound comparisons. Thus, we show for the first time the suitability of endogenous WNT/?-catenin signalling during embryonic development to provide an unambiguous and sensitive mammalian in vivo model to assess the efficacy and bioavailability of potential WNT/?-catenin antagonists.



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