Definition

An orally bioavailable, small molecule inhibitor of the auto-palmitoylation of the transcription factor TEAD (TEA domain), with potential antineoplastic activity. Upon oral administration, TEAD inhibitor VT3989 inhibits TEAD auto-palmitoylation, thereby disrupting the interaction between the transcription co-activators yes-associated protein 1 (YAP)/transcriptional coactivator with PDZ-binding motif (TAZ) and TEAD. This may inhibit YAP/TAZ-TEAD promoted gene transcription involved in tumor cell proliferation and survival. The Hippo-YAP/TAZ-TEAD pathway is dysregulated in certain cancers and diseases.