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BGI-9004 is a preclinical small molecule drug candidate being developed by BridGene Biosciences as a covalent inhibitor of the TEA Domain (TEAD) transcription factors (TEAD1-4). By targeting the Hippo signaling pathway, BGI-9004 binds to a conserved cysteine residue (Cys359) within the TEAD palmitoylation pocket, effectively disrupting the oncogenic YAP/TAZ-TEAD transcriptional complex. This inhibition leads to cell cycle arrest and apoptosis in YAP/TAZ-dependent cancer cells. Discovered via BridGene's proprietary IMTAC chemoproteomics platform, BGI-9004 has demonstrated high selectivity, favorable pharmacokinetics, and significant anti-tumor activity in preclinical models, particularly in cancers with Hippo pathway mutations such as NF2-deficient mesothelioma.
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