DIM containing peptides 3

Designer biomarker peptides have conceivable pharmacophoric features that regulates the hormonal signaling systems in several human cancers, whereas conventional small molecule inhibitors or large biologics acts restrictedly. Here, we have represented a combined approach for designing peptides with unnatural amino acid mimics, a plant hormone I3C dimer 3,3'-diindole methane (DIM). The concept involves synthesizes of DIM-peptides and is evaluated for their efficacy against hormone-dependent MCF 7 breast cancer cells. Peptides have shown significant cytotoxic activity against breast cancer cell line, while being non-toxic to normal breast cell line MCF10A. Furthermore, peptides induced cell cycle arrest, inhibited cellular migration and invasion, reduced clonogenic activity, advanced over regulated mammosphere formation, and induced programmed cell death, with low dose superior efficacy. In addition, these peptides inhibited proliferation, migration and invasion as EMT associated gene expression. In summary, we present evidence for potential hormone based therapeutic efficacy of DIM enriched small peptides against hormone estrogen receptor positive breast cancers.