EPE peptide

EPE peptide is a synthetic cell-penetrating peptide inhibitor that specifically blocks the nuclear translocation of extracellular-signal-regulated kinases 1 and 2 (ERK1/2), thereby dissociating cytosolic from nuclear ERK1/2 functions. By preventing ERK1/2 entry into the nucleus, EPE peptide inhibits the transcriptional activity and downstream effects of nuclear ERK signaling, such as cell proliferation and survival in cancer cells. Preclinical studies demonstrate that EPE peptide reduces the growth of BRAF-, NRAS-, and some NF1-mutant melanomas, induces apoptosis, and profoundly inhibits tumor progression in relevant mouse models. Its mechanism is distinct from direct ERK kinase inhibition, producing additive or synergistic effects in combination with MEK inhibitors like trametinib. EPE peptide is also being investigated as a molecular tool to dissect nuclear MAPK signaling in models of learning, memory, and neurobiology, with gene delivery strategies explored to overcome peptide delivery limitations.

Other names

EPEERK1/2 nuclear translocation inhibitor peptide