Science and Math, Singapore University of Technology & Design, Singapore; School of BioSciences, University of Melbourne, Parkville, VIC, Australia.
School of BioSciences, University of Melbourne, Parkville, VIC, Australia; Department of Physiology, Anatomy & Microbiology, La Trobe University, Bundoora, VIC, Australia.
Curr Opin Pharmacol. 2019 Apr;45:42-48. doi: 10.1016/j.coph.2019.04.001. Epub 2019 Apr 29.
Cardiovascular disease is the most common cause of mortality worldwide, accounting for almost 50% of all deaths globally. Vascular endothelial dysfunction and fibrosis are critical in the pathophysiology of cardiovascular disease. Relaxin, an insulin-like peptide, is known to have beneficial actions in the cardiovascular system through its vasoprotective and anti-fibrotic effects. However, relaxin has several limitations of peptide-based drugs such as poor oral bioavailability, laborious, and expensive to synthesize. This review will focus on recent developments in relaxin mimetics, their pharmacology, associated signalling mechanisms, and their therapeutic potential for the management and treatment of cardiovascular disease.
心血管疾病是全球最常见的死亡原因，占全球所有死亡人数的近 50%。血管内皮功能障碍和纤维化是心血管疾病病理生理学中的关键因素。松弛素是一种胰岛素样肽，已知通过其血管保护和抗纤维化作用对心血管系统具有有益作用。然而，松弛素具有基于肽的药物的几个局限性，例如口服生物利用度差、合成费力且昂贵。本综述将重点介绍松弛素类似物的最新进展、它们的药理学、相关信号机制以及它们在管理和治疗心血管疾病方面的治疗潜力。
