VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts the interaction between YAP/TAZ and TEAD via inhibition of TEAD1 (IC50 = 1 nM).1 It prevented TAC-induced cardiac hypertrophy and dysfunction in WT mice by blocking the interaction of TEAD1 with BRD4.2 VT103 enhanced the efficacy of dabrafenib in KTOR81 lung adenocarcinoma cells and xenograft models.3 VT103 acts a molecular glue between TEAD and the transcriptional repressor VGLL4 leading to antagonism of YAP activity.4
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