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[Dmt1, D-2-Nal4]endomorphin-1 is a synthetic tetrapeptide analogue of the endogenous opioid endomorphin-1. It is modified with 2',6'-dimethyl-L-tyrosine (Dmt) at the first position and D-2-naphthylalanine (D-2-Nal) at the fourth position. Unlike the parent peptide, which is a potent mu-opioid receptor (MOR) agonist, this modified analogue functions as a selective MOR antagonist. Preclinical research has demonstrated that [Dmt1, D-2-Nal4]endomorphin-1 can up-regulate MOR gene expression and inhibit the proliferation of MCF-7 breast cancer cells, suggesting its utility as a research tool for investigating opioid signaling pathways and their role in tumor biology.
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