Shandong Provincial Key Laboratory of Animal Cell and Developmental Biology, School of Life Sciences, Shandong University, Qingdao 266237, China.
Department of Anatomy, Physiology and Pharmacology, College of Veterinary Medicine, Auburn University, Auburn, AL 36849, USA.
Int J Mol Sci. 2022 Aug 5;23(15):8727. doi: 10.3390/ijms23158727.
As the most recent melanocortin receptor (MCR) identified, melanocortin-5 receptor (MC5R) has unique tissue expression patterns, pharmacological properties, and physiological functions. Different from the other four MCR subtypes, MC5R is widely distributed in both the central nervous system and peripheral tissues and is associated with multiple functions. MC5R in sebaceous and preputial glands regulates lipid production and sexual behavior, respectively. MC5R expressed in immune cells is involved in immunomodulation. Among the five MCRs, MC5R is the predominant subtype expressed in skeletal muscle and white adipose tissue, tissues critical for energy metabolism. Activated MC5R triggers lipid mobilization in adipocytes and glucose uptake in skeletal muscle. Therefore, MC5R is a potential target for treating patients with obesity and diabetes mellitus. Melanocortin-2 receptor accessory proteins can modulate the cell surface expression, dimerization, and pharmacology of MC5R. This minireview summarizes the molecular and pharmacological properties of MC5R and highlights the progress made on MC5R in energy metabolism. We poInt. out knowledge gaps that need to be explored in the future.
作为最新发现的黑色素皮质素受体（MCR）之一，黑色素皮质素-5 受体（MC5R）具有独特的组织表达模式、药理学特性和生理功能。与其他四种 MCR 亚型不同，MC5R 广泛分布于中枢神经系统和外周组织，并与多种功能相关。皮脂腺和包皮中的 MC5R 分别调节脂质产生和性行为。表达在免疫细胞中的 MC5R 参与免疫调节。在这五个 MCR 中，MC5R 是骨骼肌和白色脂肪组织中表达最丰富的亚型，这些组织对能量代谢至关重要。激活的 MC5R 触发脂肪细胞中的脂质动员和骨骼肌中的葡萄糖摄取。因此，MC5R 是治疗肥胖症和糖尿病患者的潜在靶点。黑色素皮质素-2 受体辅助蛋白可以调节 MC5R 的细胞表面表达、二聚化和药理学。这篇综述总结了 MC5R 的分子和药理学特性，并强调了在能量代谢方面 MC5R 的研究进展。我们指出了未来需要探索的知识空白。
