Article: Identification of a Quinone Derivative as a YAP/TEAD Activity Modulator from a Repurposing Library.
2022 Volume 14, Issue 2
Abstract: The transcriptional regulators YAP (Yes-associated protein) and TAZ (transcriptional co-activator with PDZ-binding motif) are the major downstream effectors in the Hippo pathway and are involved in cancer progression through modulation of the activity of ...
Abstract | The transcriptional regulators YAP (Yes-associated protein) and TAZ (transcriptional co-activator with PDZ-binding motif) are the major downstream effectors in the Hippo pathway and are involved in cancer progression through modulation of the activity of TEAD (transcriptional enhanced associate domain) transcription factors. To exploit the advantages of drug repurposing in the search of new drugs, we developed a similar approach for the identification of new hits interfering with TEAD target gene expression. In our study, a 27-member in-house library was assembled, characterized, and screened for its cancer cell growth inhibition effect. In a secondary luciferase-based assay, only seven compounds confirmed their specific involvement in TEAD activity. |
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Language | English |
Publishing date | 2022-02-10 |
Publishing country | Switzerland |
Document type | Journal Article |
ZDB-ID | 2527217-2 |
ISSN | 1999-4923 |
ISSN | 1999-4923 |
DOI | 10.3390/pharmaceutics14020391 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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