Design, Synthesis and Evaluation of a Series of 1,5-Diaryl-1,2,3-triazole-4-carbohydrazones as Inhibitors of the YAP-TAZ/TEAD Complex. Bailly, F., Gibault, F., Sturbaut, M., Coevoet, M., Pugnière, M., Burtscher, A., Allemand, F., Melnyk, P., Hong, W., Rubin, B. P., Pobbati, A. V., Guichou, J., & Cotelle, P. ChemMedChem. _eprint: https://chemistry-europe.onlinelibrary.wiley.com/doi/pdf/10.1002/cmdc.202100153![Design, Synthesis and Evaluation of a Series of 1,5-Diaryl-1,2,3-triazole-4-carbohydrazones as Inhibitors of the YAP-TAZ/TEAD Complex [link]](https://bibbase.org/img/filetypes/link.svg "link")
Paper doi abstract bibtex Starting from our previously reported hit, a series of 1,5-diaryl-1,2,3-triazole-4-carbohydrazones was synthesized and evaluated as inhibitors of the YAP/TAZ-TEAD complex. Binding to hTEAD2 of our compounds was evidenced by nanodifferential scanning fluorimetry and they were also shown by polarization fluorescence to disrupt to some extent YAP-TEAD interaction. They displayed micromolar inhibition in a luciferase gene reporter assay in transfected HEK293T cells and decreased mRNAs levels of TEAD target genes measured by RTqPCR in MDA-MB231 cells. In spite of limiting cytotoxicities, careful analysis of the biological data let emerge some new hits as the starting points for future design aimed at improving YAP-TEAD disruption.
@article{bailly_design_nodate,
title = {Design, {Synthesis} and {Evaluation} of a {Series} of 1,5-{Diaryl}-1,2,3-triazole-4-carbohydrazones as {Inhibitors} of the {YAP}-{TAZ}/{TEAD} {Complex}},
volume = {n/a},
copyright = {© 2021 Wiley-VCH GmbH},
issn = {1860-7187},
url = {https://chemistry-europe.onlinelibrary.wiley.com/doi/abs/10.1002/cmdc.202100153},
doi = {https://doi.org/10.1002/cmdc.202100153},
abstract = {Starting from our previously reported hit, a series of 1,5-diaryl-1,2,3-triazole-4-carbohydrazones was synthesized and evaluated as inhibitors of the YAP/TAZ-TEAD complex. Binding to hTEAD2 of our compounds was evidenced by nanodifferential scanning fluorimetry and they were also shown by polarization fluorescence to disrupt to some extent YAP-TEAD interaction. They displayed micromolar inhibition in a luciferase gene reporter assay in transfected HEK293T cells and decreased mRNAs levels of TEAD target genes measured by RTqPCR in MDA-MB231 cells. In spite of limiting cytotoxicities, careful analysis of the biological data let emerge some new hits as the starting points for future design aimed at improving YAP-TEAD disruption.},
language = {en},
number = {n/a},
urldate = {2021-06-06},
journal = {ChemMedChem},
author = {Bailly, Fabrice and Gibault, Floriane and Sturbaut, Manon and Coevoet, Mathilde and Pugnière, Martine and Burtscher, Ashley and Allemand, Frédéric and Melnyk, Patricia and Hong, Wanjin and Rubin, Brian P. and Pobbati, Ajaybabu V. and Guichou, Jean-François and Cotelle, Philippe},
note = {\_eprint: https://chemistry-europe.onlinelibrary.wiley.com/doi/pdf/10.1002/cmdc.202100153},
keywords = {Hippo pathway, TEAD binding, YAP-TEAD inhibition, antitumor agents, protein-protein interactions},
}
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V.","Guichou, J.","Cotelle, P."],"bibdata":{"bibtype":"article","type":"article","title":"Design, Synthesis and Evaluation of a Series of 1,5-Diaryl-1,2,3-triazole-4-carbohydrazones as Inhibitors of the YAP-TAZ/TEAD Complex","volume":"n/a","copyright":"© 2021 Wiley-VCH GmbH","issn":"1860-7187","url":"https://chemistry-europe.onlinelibrary.wiley.com/doi/abs/10.1002/cmdc.202100153","doi":"https://doi.org/10.1002/cmdc.202100153","abstract":"Starting from our previously reported hit, a series of 1,5-diaryl-1,2,3-triazole-4-carbohydrazones was synthesized and evaluated as inhibitors of the YAP/TAZ-TEAD complex. Binding to hTEAD2 of our compounds was evidenced by nanodifferential scanning fluorimetry and they were also shown by polarization fluorescence to disrupt to some extent YAP-TEAD interaction. They displayed micromolar inhibition in a luciferase gene reporter assay in transfected HEK293T cells and decreased mRNAs levels of TEAD target genes measured by RTqPCR in MDA-MB231 cells. 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Binding to hTEAD2 of our compounds was evidenced by nanodifferential scanning fluorimetry and they were also shown by polarization fluorescence to disrupt to some extent YAP-TEAD interaction. They displayed micromolar inhibition in a luciferase gene reporter assay in transfected HEK293T cells and decreased mRNAs levels of TEAD target genes measured by RTqPCR in MDA-MB231 cells. 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