selective TEAD1 inhibitor

Selective TEAD1 inhibitors are a class of small molecule therapeutics designed to target the TEA Domain (TEAD) transcription factor family, specifically the TEAD1 isoform. These inhibitors function by disrupting the interaction between TEAD1 and its transcriptional co-activators, YAP (Yes-associated protein) and TAZ (Transcriptional co-activator with PDZ-binding motif). This interaction is a critical downstream component of the Hippo signaling pathway, which is frequently dysregulated in various cancers, such as malignant mesothelioma and NF2-mutant solid tumors. By preventing the formation of the YAP/TAZ-TEAD complex, these inhibitors suppress the expression of pro-survival and pro-proliferative genes (e.g., CTGF, CYR61), thereby inhibiting tumor growth. Selective TEAD1 inhibitors are often compared to pan-TEAD or multi-isoform (e.g., TEAD1/3) inhibitors to evaluate efficacy and safety profiles across different Hippo-altered genetic backgrounds.

Other names

selective TEAD1 inhibitorTEAD1 inhibitorTEAD-1 inhibitorTEAD 1 inhibitor