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YAP-TEAD inhibitor
- Development stage
- Preclinical
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
YAP-TEAD inhibitors are a class of targeted therapies designed to disrupt the interaction between the transcriptional co-activator YAP (Yes-associated protein) and the TEAD (TEA domain) family of transcription factors. This interaction is a critical downstream component of the Hippo signaling pathway, which regulates cell proliferation, apoptosis, and organ size. Dysregulation of this pathway, often through loss of tumor suppressors like NF2 or NUMB, leads to YAP hyperactivation and the transcription of genes promoting epithelial-mesenchymal transition (EMT), survival, and chemoresistance. These inhibitors are being investigated for the treatment of various solid tumors, including mesothelioma, schwannoma, and bladder cancer, particularly those with specific genetic alterations that drive YAP-dependent growth.
- Other names
- YAP/TEAD inhibitorYAP-TEAD interaction inhibitorHippo pathway inhibitor
02
Targets
TEAD1TEAD3TEAD2 (TEA domain family member 2)TEAD4
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