Interface 3 of the YAP:TEAD complex a key Hippo pathway effector driving oncogenesis. • A robust fluorescence anisotropy displacement assay was developed using an Ω-loop peptide probe to identify TEAD4 Interface 3 inhibitors. • Successful probe displacement by pyrazolopiperidone inhibitors confirms the assay’s suitability for hit and lead screening.
Targeting the YAP:TEAD domain through fluorescence-anisotropy displacement assay
Davide Illuminati;Salvatore Pacifico;Remo Guerrini;Marco Mor;Maria Paola Costi
2026
Abstract
Interface 3 of the YAP:TEAD complex a key Hippo pathway effector driving oncogenesis. • A robust fluorescence anisotropy displacement assay was developed using an Ω-loop peptide probe to identify TEAD4 Interface 3 inhibitors. • Successful probe displacement by pyrazolopiperidone inhibitors confirms the assay’s suitability for hit and lead screening.File in questo prodotto:
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