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Pi-CARM1-TAT is a cell-permeable peptide inhibitor designed to target Coactivator-associated arginine methyltransferase 1 (CARM1), also known as PRMT4. CARM1 is an epigenetic modulator that plays a pivotal role in the progression of various cancers, particularly breast cancer, by regulating the expression of oncogenic estrogen receptor alpha (ERα) target genes and type I interferon-induced genes. The peptide consists of the Pi-CARM1 inhibitor sequence conjugated to the Trans-Activator of Transcription (TAT) cell-penetrating peptide to facilitate intracellular delivery. In preclinical models, Pi-CARM1-TAT has demonstrated the ability to suppress breast cancer cell proliferation, reduce tumor growth, and overcome resistance to endocrine therapies. It also exhibits synergistic effects when combined with standard treatments like etoposide or endocrine therapy drugs.
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