Optimization of a Class of Dihydrobenzofurane Analogs toward Orally Efficacious YAP‐TEAD Protein‐Protein Interaction Inhibitors
Sign Up to like & getrecommendations! Published in 2023 at "ChemMedChem"
DOI: 10.1002/cmdc.202300051
Abstract: The inhibition of the YAP‐TEAD protein‐protein interaction constitutes a promising therapeutic approach for the treatment of cancers linked to the dysregulation of the Hippo signaling pathway. The identification of a class of small molecules which… read more here.
Keywords: interaction; protein protein; protein interaction; class ... See more keywords
CDX2 downregulation in mouse mural trophectoderm during peri‐implantation is heteronomous, dependent on the YAP‐TEAD pathway and controlled by estrogen‐induced factors
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DOI: 10.1002/rmb2.12446
Abstract: Abstract Purpose To investigate the transition of CDX2 expression patterns in mouse trophectoderm (TE) and its regulatory mechanisms during implantation. Methods Mouse E3.5–4.5 blastocysts were used to immunostain CDX2, YAP, TEAD4, and ESRRB. Endogenous estrogen… read more here.
Keywords: cdx2 downregulation; yap tead; cdx2 expression; estrogen ... See more keywords
YAP as a therapeutic target to reverse trastuzumab resistance
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DOI: 10.1007/s10120-025-01630-w
Abstract: Trastuzumab resistance in HER2-positive cancers remains a significant clinical challenge with limited therapeutic options. Although the tumor-promoting role of the Yes-associated protein (YAP) pathway is well established, its role in trastuzumab resistance remains unclear. We… read more here.
Keywords: trastuzumab resistance; yap; her2; trastuzumab ... See more keywords
Neural Progenitor Cells Undergoing Yap/Tead-Mediated Enhanced Self-Renewal Form Heterotopias More Easily in the Diencephalon than in the Telencephalon
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DOI: 10.1007/s11064-017-2390-x
Abstract: Spatiotemporally ordered production of cells is essential for brain development. Normally, most undifferentiated neural progenitor cells (NPCs) face the apical (ventricular) surface of embryonic brain walls. Pathological detachment of NPCs from the apical surface and… read more here.
Keywords: neural progenitor; progenitor cells; tead; yap tead ... See more keywords
Leveraging Advanced In Silico Techniques in Early Drug Discovery: A Study of Potent Small-Molecule YAP-TEAD PPI Disruptors
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DOI: 10.1021/acs.jcim.3c00122
Abstract: Disruption of the YAP-TEAD protein-protein interaction is an attractive therapeutic strategy in oncology to suppress tumor progression and cancer metastasis. YAP binds to TEAD at a large flat binding interface (∼3500 Å2) devoid of a… read more here.
Keywords: yap tead; drug; discovery; small molecule ... See more keywords
YAP/TEAD4/SP1-induced VISTA expression as a tumor cell-intrinsic mechanism of immunosuppression in colorectal cancer
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DOI: 10.1038/s41418-025-01446-2
Abstract: Hyperactivation of the YAP/TEAD transcriptional complex in cancers facilitates the development of an immunosuppressive tumor microenvironment. Herein, we observed that the transcription factor SP1 physically interacts with and stabilizes the YAP/TEAD complex at regulatory genomic… read more here.
Keywords: sp1; yap; tumor; cell ... See more keywords
EXTH-51. ANTI-INVASIVE EFFICACY AND SURVIVAL BENEFIT OF THE YAP-TEAD INHIBITOR VERTEPORFIN IN PRECLINICAL GLIOBLASTOMA MODELS
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DOI: 10.1093/neuonc/noaa215.405
Abstract: Glioblastoma (GBM) remains an incurable disease, in large part due to its malignant infiltrative spread, and current clinical therapy fails to target the invasive nature of tumor cells in disease progression and recurrence. Here, we… read more here.
Keywords: tumor; survival benefit; gbm; yap tead ... See more keywords
Abstract 4491: TY-0584: A potent, orally available small molecule YAP/TEAD inhibitor, exhibits anti-tumor effects in vitro and in vivo
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-4491
Abstract: Hippo/YAP pathway plays an essential role in cell proliferation, tissue regeneration, and tumorigenesis. The emerging evidence shows that hyperactivation of the Hippo/YAP pathway induces metastasis, chemoresistance, and the attribute of cancer stem cells. Dysregulated Hippo/YAP… read more here.
Keywords: inhibitor; yap tead; yap; tead inhibitor ... See more keywords
Abstract 6778: Targeting the YAP-TEAD interaction in brain metastatic breast cancer cells
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DOI: 10.1158/1538-7445.am2025-6778
Abstract: Breast cancer metastasis to the brain is a devastating stage of breast cancer that presents with cognitive decline and seizures, and currently there are no treatments available. Brain metastases are resistant to immunotherapy, chemotherapy, and… read more here.
Keywords: cancer; breast cancer; cancer cells; brain ... See more keywords
Abstract B020: Identification of VASP as a glucose-sensitive YAP-TEAD target gene in a human triple-negative breast cancer cell line
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DOI: 10.1158/1538-7445.canevol25-b020
Abstract: Triple-negative breast cancer (TNBC) is an aggressive subtype that lacks targeted therapies, highlighting the urgent need for novel treatment strategies. Clinical evidence shows that TNBC patients with metabolic dysregulation—such as obesity or diabetes, often accompanied… read more here.
Keywords: cancer; breast cancer; target gene; cancer cell ... See more keywords
Abstract A28: DEAD-box RNA helicase DP103 enhances YAP sumoylation for YAP-TEAD dependence and statin sensitivity in triple-negative breast cancer
Sign Up to like & getrecommendations! Published in 2020 at "Molecular Cancer Research"
DOI: 10.1158/1557-3125.hippo19-a28
Abstract: Simvastatin (SMV), a lipophilic statin used for lowering cholesterol, inhibits 3-hydroxy-3-methylglutaryl-CoA reductase (HMGCR), the key enzyme of the mevalonate pathway. Studies have shown that cancer cells express deregulated level of HMGCR and statins exert antitumoral… read more here.
Keywords: sumoylation yap; breast cancer; dp103; yap tead ... See more keywords