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Br J Dermatol. 2019 Jan 13. doi: 10.1111/bjd.17634. [Epub ahead of print]

Identification of small peptides and glycinamide that inhibit melanin synthesis using a positional scanning synthetic peptide combinatorial library.

Author information

1
Department of Molecular Medicine, Cell and Matrix Research Institute, BK21 Plus KNU Biomedical Convergence Program, School of Medicine, Kyungpook National University, 680 Gukchaebosang-ro, Jung-gu, Daegu, 41944, Republic of Korea.
2
Ruby Crown Co., Ltd., Suite 505, Korea Mediventure Center, 76 Dongnae-ro, Dong-gu, Daegu, 41061, Republic of Korea.

Abstract

BACKGROUND:

Antimelanogenic peptides are potentially useful to treat hyperpigmentation, but many peptides have limited application because of high cost and/or low activity.

OBJECTIVES:

To identify small and potent peptide inhibitors of cellular melanin synthesis useful for cosmetic and medical applications.

METHODS:

A positional scanning synthetic tetrapeptide combinatorial library was used for screening of potentially active peptides. Antimelanogenic activities of the peptide pools and individual peptides were evaluated in B16-F10 melanoma cells and human epidermal melanocytes (HEMs) treated with alpha-melanocyte-stimulating hormone (α-MSH).

RESULTS:

The predicted active tetrapeptide sequences were R-(F/L)-(C/W)-(G/R)-NH2 . Of the individual tetrapeptides tested, D3 (RFWG-NH2 ) and D5 (RLWG-NH2 ) exhibited high antimelanogenic activities. Tetrapeptide D9 (FRWG-NH2 ) with a sequence identical to that of a portion of α-MSH also showed antimelanogenic activity. Of the tripeptides tested, E5 (FWG-NH2 ), E6 (LWG-NH2 ), and E7 (RWG-NH2 ) were relatively more active. Dipeptide F1 (WG-NH2 ) and monopeptide G1 (G-NH2 , glycinamide) retained activity, but G2 (Ac-G-NH2 ) and G3 (glycine) did not. The antimelanogenic activities of peptides D3, E5, F1, and G1 were verified in α-MSH-stimulated HEMs. Commercially available G-NH2 ·HCl suppressed the phosphorylation levels of cAMP-responsive element binding protein, protein levels of microphthalmia-associated transcription factor and tyrosinase, L-tyrosine hydroxylase activity of tyrosinase, and the melanin levels in stimulated cells.

CONCLUSIONS:

Small peptides, including glycinamide and tryptophanyl glycinamide, are potent antimelanogenic agents with potential value for the treatment of skin hyperpigmentation. This article is protected by copyright. All rights reserved.

KEYWORDS:

Glycinamide; Melanin; Melanocortin 1 receptor; Melanocytes; Peptide; α-Melanocyte-stimulating hormone

PMID:
30637717
DOI:
10.1111/bjd.17634

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