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MYC TAD disruptor is a preclinical-stage biologic therapeutic being developed by Grove Biopharma. It is designed to inhibit the activity of the MYC transcription factor, a central driver in many human cancers that has historically been considered undruggable due to its lack of a defined small-molecule binding pocket. The drug specifically targets the MYC transactivation domain (TAD), disrupting critical protein-protein interactions required for its oncogenic function. These include the interaction between c-Myc and the PNUTS/PP1 (Protein Phosphatase 1) complex, as well as the interaction between N-Myc and Aurora kinase A (Aurora-A). By preventing the formation of these complexes, the disruptor molecule aims to suppress MYC-mediated gene transcription and induce tumor regression. The program is currently in the lead generation phase of preclinical development for MYC-driven malignancies, including neuroblastoma, medulloblastoma, acute myeloid leukemia (AML), and neuroendocrine prostate cancer.
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