TY - JOUR
T1 - MC1R Peptide Agonist Self-Assembles into a Hydrogel That Promotes Skin Pigmentation for Treating Vitiligo
AU - Zhu, Ci
AU - Li, Tingting
AU - Wang, Zhuole
AU - Li, Zenghui
AU - Wei, Jiaying
AU - Han, Hong
AU - Yuan, Dan
AU - Cai, Minying
AU - Shi, Junfeng
N1 - Publisher Copyright:
© 2023 American Chemical Society.
PY - 2023/5/9
Y1 - 2023/5/9
N2 - Vitiligo, a common skin disease that seriously affects 0.5-2.0% of the worldwide population, lacks approved therapeutics due to a wide range of adverse side effects. As a key regulator of skin pigmentation, MC1R may be an effective therapeutic target for vitiligo. Herein, we report an MC1R peptide agonist that directly self-assembles into nanofibrils that form a hydrogel matrix under normal physiological conditions. This hydrogel exhibits higher stability than free peptides, sustained release, rapid recovery from shear-thinning, and resistance to enzymatic proteolysis. Furthermore, this peptidal MC1R agonist upregulates tyrosinase, tyrosinase-related protein-1 (TYRP-1), and tyrosinase-related protein-2 (TYRP-2) to stimulate melanin synthesis. More importantly, MC1R agonist hydrogel promotes skin pigmentation in mice more potently than free MC1R agonist. This study supports the development of this MC1R agonist hydrogel as a promising pharmacological intervention for vitiligo.
AB - Vitiligo, a common skin disease that seriously affects 0.5-2.0% of the worldwide population, lacks approved therapeutics due to a wide range of adverse side effects. As a key regulator of skin pigmentation, MC1R may be an effective therapeutic target for vitiligo. Herein, we report an MC1R peptide agonist that directly self-assembles into nanofibrils that form a hydrogel matrix under normal physiological conditions. This hydrogel exhibits higher stability than free peptides, sustained release, rapid recovery from shear-thinning, and resistance to enzymatic proteolysis. Furthermore, this peptidal MC1R agonist upregulates tyrosinase, tyrosinase-related protein-1 (TYRP-1), and tyrosinase-related protein-2 (TYRP-2) to stimulate melanin synthesis. More importantly, MC1R agonist hydrogel promotes skin pigmentation in mice more potently than free MC1R agonist. This study supports the development of this MC1R agonist hydrogel as a promising pharmacological intervention for vitiligo.
KW - melanocortin 1 receptor
KW - peptide drug
KW - peptide self-assembly
KW - supramolecular hydrogel
KW - vitiligo
UR - http://www.scopus.com/inward/record.url?scp=85156215709&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85156215709&partnerID=8YFLogxK
U2 - 10.1021/acsnano.3c01960
DO - 10.1021/acsnano.3c01960
M3 - Article
C2 - 37115703
AN - SCOPUS:85156215709
SN - 1936-0851
VL - 17
SP - 8723
EP - 8733
JO - ACS Nano
JF - ACS Nano
IS - 9
ER -