D-arginine peptide

D-arginine peptide (D-Arg PEP) is a modified 7-mer peptide derived from L-penetratin, designed to target and inhibit the activating transcription factors E2F1, E2F2, and E2F3. By binding tightly to E2F promoters, the peptide suppresses the transcription of genes essential for DNA synthesis, cellular proliferation, and tumor growth. The substitution of L-arginine with D-arginine enhances the peptide's stability against serum proteases and increases its potency. To further improve in vivo stability and delivery, the peptide has been encapsulated in PEGylated liposomes (PL-PEP). Developed by researchers at the Rutgers Cancer Institute of New Jersey, this therapeutic candidate has demonstrated synergistic anti-tumor activity when combined with DNA-damaging agents like cisplatin or antimetabolites like pemetrexed in preclinical models of prostate, lung, and breast cancers.

Other names

D-arginine modified penetratin peptideD-Arg modified E2F-targeting peptide