College of Pharmacy, Gachon University, 191 Hambakmoe-ro, Yeonsu-gu, Incheon 21936, Republic of Korea.
Gachon Pharmaceutical Research Institute, Gachon University, 191 Hambakmoe-ro, Yeonsu-gu, Incheon 21936, Republic of Korea.
Int J Mol Sci. 2023 Jul 29;24(15):12152. doi: 10.3390/ijms241512152.
Melanocortins play crucial roles in regulating the stress response, inflammation, and skin pigmentation. In this review, we focus on the melanocortin 1 receptor (MC1R), a G protein-coupled receptor primarily known for regulating skin pigmentation and exhibiting anti-inflammatory effects. First, we provide an overview of the structure, signaling pathways, and related diseases of MC1R. Next, we discuss the potential therapeutic use of synthetic peptides and small molecule modulators of MC1R, highlighting the development of various drugs that enhance stability through amino acid sequence modifications and small molecule drugs to overcome limitations associated with peptide characteristics. Notably, MC1R-targeted drugs have applications beyond skin pigmentation-related diseases, which predominantly affect MC1R in melanocytes. These drugs can also be useful in treating inflammatory diseases with MC1R expression present in various cells. Our review underscores the potential of MC1R-targeted drugs to treat a wide range of diseases and encourages further research in this area.
黑素细胞刺激素在调节应激反应、炎症和皮肤色素沉着方面发挥着关键作用。在这篇综述中,我们重点介绍黑素细胞刺激素 1 受体(MC1R),它是一种 G 蛋白偶联受体,主要负责调节皮肤色素沉着,并具有抗炎作用。首先,我们提供了 MC1R 的结构、信号通路和相关疾病的概述。接下来,我们讨论了合成肽和 MC1R 小分子调节剂的潜在治疗用途,重点介绍了通过氨基酸序列修饰和小分子药物来提高稳定性的各种药物的开发,以克服与肽特性相关的限制。值得注意的是,MC1R 靶向药物的应用不仅限于与皮肤色素沉着相关的疾病,这些疾病主要影响黑素细胞中的 MC1R。这些药物在治疗各种细胞中表达 MC1R 的炎症性疾病方面也可能很有用。我们的综述强调了 MC1R 靶向药物治疗广泛疾病的潜力,并鼓励在该领域进行进一步研究。