Structural optimization of pep7, a small peptide extracted from epimorphin, for effective induction of hair follicle anagen

In 2005, Hirai, Takebe, and Nakajima conducted a study to enhance the hair follicle anagen-inducing ability of a small peptide, pep7, derived from epimorphin. They discovered that modifying pep7 by removing three amino acids at the C-terminus, replacing the seventh amino acid with Alanine, and adding an intramolecular disulfide bridge, significantly increased its activity. The resulting peptide, named EPM peptide, had a molecular weight of 950 Da and was effective at very low concentrations, even below 0.00001%. The EPM peptide's hair follicle regeneration effects were amplified when used with 1% minoxidil. The study also involved creating a mutation library and screening for active derivatives, with the EPM peptide showing the highest activity in vitro and effectively inducing the anagen phase in vivo in C57BL mice. The EPM peptide binds directly to hair follicle epithelia, has a distinct functional pathway from minoxidil, and the combination of both agents induced a more rapid transition to the anagen stage than minoxidil alone. The study did not specify the number of subjects but suggested that the EPM peptide could be a cost-effective and low-side-effect option for clinical hair regeneration applications, with further studies needed to assess its clinical applicability.