Minireview: Peptide Analogs and Short Sequence Oligopeptides as Modulators of Skin Pigmentation
Anan Abu Ubeid and Basil M. Hantash
Affiliation: Escape Therapeutics, Inc., 5941 Optical Court, San Jose, CA 95138, USA.
Short sequence amino acids or oligopeptides have recently garnered attention for use as treatments for a myriad
of dermatologic disorders due to their ability to effect and modulate various biological processes in the epidermis and
dermis, rendering them promising candidates as medical and cosmeceutical therapeutics. Major advantages include their
relative ease of synthesis and multitude of modifications that can be applied to enhance potency, affinity, specificity, hydrophilicity
or hydrophobicity and cytotoxicity. Given the photoprotective effects of eumelanin on skin, there has been
substantial interest in developing agents, particularly α-MSH analogs, that can induce ‘sunless tanning’ helping reduce
risk of melanoma and non-melanoma skin cancer. In this mini review, we present some of the recent and leading peptide
modulators of melanogenesis with relevant clinical data and medical indications. Short sequence oligopeptides with tyrosinase
inhibitory activity that can significantly reduce hyperpigmentation, as well α-MSH analogs that can enhance
eumelanogenesis, are currently being clinically tested for treatment of erythropoietic protoporphyria, polymorphous light
eruption, solar urticaria, actinic keratosis, and “sunless tanning”. Success in developing such products can help reduce the
incidence of skin cancer, one that surpasses that of all other human cancers combined.
Keywords: α-MSH analogs, hyperpigmentation, hypopigmentation, melanocortin 1 receptor, melanogenesis, tyrosinase.
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