GNE-7883

GNE-7883 is a small molecule inhibitor of the TEA Domain (TEAD) transcription factors, which are the primary nuclear effectors of the Hippo signaling pathway. It functions by binding to the TEAD palmitoylation pocket, thereby disrupting the transcriptional activity of the YAP/TAZ-TEAD complex. This complex is frequently upregulated in various malignancies and contributes to therapy resistance, cell proliferation, and metastasis. Preclinical studies have demonstrated that GNE-7883 can suppress growth and invasiveness in models of castration-resistant prostate cancer, including those resistant to enzalutamide, by downregulating Hippo pathway target genes and potentially modulating PD-L1 expression.