MC1R Peptide Agonist Self-Assembles into a Hydrogel That Promotes Skin Pigmentation for Treating Vitiligo,ACS Nano

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MC1R Peptide Agonist Self-Assembles into a Hydrogel That Promotes Skin Pigmentation for Treating Vitiligo
ACS Nano ( IF 15.8 ) Pub Date : 2023-04-28 , DOI: 10.1021/acsnano.3c01960
Ci Zhu ₁ , Tingting Li ₁ , Zhuole Wang ₁ , Zenghui Li ₁ , Jiaying Wei ₁ , Hong Han ₁ , Dan Yuan _{1,

2} , Minying Cai ₃ , Junfeng Shi _{1,

2}

Affiliation

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.

中文翻译：

MC1R 肽激动剂自组装成水凝胶促进皮肤色素沉着治疗白斑

白癜风是一种常见的皮肤病，严重影响全球 0.5-2.0% 的人口，由于广泛的不良副作用，缺乏批准的治疗方法。作为皮肤色素沉着的关键调节剂，MC1R可能是白斑病的有效治疗靶点。在此，我们报告了一种 MC1R 肽激动剂，它在正常生理条件下直接自组装成纳米纤维，形成水凝胶基质。这种水凝胶表现出比游离肽更高的稳定性、持续释放、从剪切稀化中快速恢复以及对酶促蛋白水解的抗性。此外，这种肽 MC1R 激动剂上调酪氨酸酶、酪氨酸酶相关蛋白 1 (TYRP-1) 和酪氨酸酶相关蛋白 2 (TYRP-2) 以刺激黑色素合成。更重要的是，MC1R 激动剂水凝胶比游离 MC1R 激动剂更有效地促进小鼠皮肤色素沉着。这项研究支持开发这种 MC1R 激动剂水凝胶作为一种有前途的白癜风药物干预。

更新日期：2023-04-28

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