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
Sign Up to like & getrecommendations! Published in 2022 at "Reproductive Medicine and Biology"
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
Neural Progenitor Cells Undergoing Yap/Tead-Mediated Enhanced Self-Renewal Form Heterotopias More Easily in the Diencephalon than in the Telencephalon
Sign Up to like & getrecommendations! Published in 2017 at "Neurochemical Research"
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
Sign Up to like & getrecommendations! Published in 2023 at "Journal of chemical information and modeling"
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
EXTH-51. ANTI-INVASIVE EFFICACY AND SURVIVAL BENEFIT OF THE YAP-TEAD INHIBITOR VERTEPORFIN IN PRECLINICAL GLIOBLASTOMA MODELS
Sign Up to like & getrecommendations! Published in 2020 at "Neuro-oncology"
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 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
Regulation of Transcription Factor YAP-TEAD by Non-coding RNA LINC00857 and the Inhibitory Effects on Ovarian Cancer Cell Proliferation.
Sign Up to like & getrecommendations! Published in 2022 at "Cellular and molecular biology"
DOI: 10.14715/cmb/2022.68.2.23
Abstract: This study was aimed to explore the expression and mechanism of the transcription factor YAP-TEAD in the Hippo signaling pathway under the regulation of non-coding Ribonucleic Acid (RNA) LINC00857 in the proliferation of ovarian cancer… read more here.
Keywords: proliferation; yap tead; factor yap; transcription factor ... See more keywords
Adaptation of the bound intrinsically disordered protein YAP to mutations at the YAP:TEAD interface.
Sign Up to like & getrecommendations! Published in 2018 at "Protein Science"
DOI: 10.2210/pdb6geg/pdb
Abstract: Many interactions between proteins are mediated by intrinsically disordered regions (IDRs). Intrinsically disordered proteins (IDPs) do not adopt a stable three-dimensional structure in their unbound form, but they become more structured upon binding to their… read more here.
Keywords: tead interface; yap tead; yap; adaptation ... See more keywords
FSH Regulates YAP-TEAD Transcriptional Activity in Bovine Granulosa Cells to Allow the Future Dominant Follicle to Exert Its Augmented Estrogenic Capacity
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms232214160
Abstract: The molecular mechanisms that drive the granulosa cells’ (GC) differentiation into a more estrogenic phenotype during follicular divergence and establishment of follicle dominance have not been completely elucidated. The main Hippo signaling effector, YAP, has,… read more here.
Keywords: dominant follicle; transcriptional activity; yap tead; bovine ... See more keywords
Covalent disruptor of YAP-TEAD association suppresses defective Hippo signaling
Sign Up to like & getrecommendations! Published in 2022 at "eLife"
DOI: 10.7554/elife.78810
Abstract: The transcription factor TEAD, together with its coactivator YAP/TAZ, is a key transcriptional modulator of the Hippo pathway. Activation of TEAD transcription by YAP has been implicated in a number of malignancies, and this complex… read more here.
Keywords: association suppresses; yap tead; yap; tead association ... See more keywords