Foster Simon R, Roura Eugeni, Molenaar Peter, Thomas Walter G
School of Biomedical Sciences, University of Queensland, St Lucia Campus, 4072, Brisbane, Australia.
Centre for Nutrition & Food Sciences, Queensland Alliance for Agriculture and Food Innovation, University of Queensland, St Lucia Campus, Brisbane, Australia.
Biophys Rev. 2015 Mar;7(1):77-89. doi: 10.1007/s12551-014-0154-2. Epub 2015 Jan 13.
G protein-coupled receptors (GPCRs) are seven-transmembrane-spanning proteins that mediate cellular and physiological responses. They are critical for cardiovascular function and are targeted for the treatment of hypertension and heart failure. Nevertheless, current therapies only target a small fraction of the cardiac GPCR repertoire, indicating that there are many opportunities to investigate unappreciated aspects of heart biology. Here, we offer an update on the contemporary view of GPCRs and the complexities of their signalling, and review the roles of the 'classical' GPCRs in cardiovascular physiology and disease. We then provide insights into other GPCRs that have been less extensively studied in the heart, including orphan, odorant and taste receptors. We contend that these novel cardiac GPCRs contribute to heart function in health and disease and thereby offer exciting opportunities to therapeutically modulate heart function.
G蛋白偶联受体(GPCRs)是介导细胞和生理反应的七次跨膜蛋白。它们对心血管功能至关重要,是高血压和心力衰竭治疗的靶点。然而,目前的治疗方法仅针对心脏GPCR库中的一小部分,这表明有很多机会去研究心脏生物学中尚未被认识的方面。在此,我们提供关于GPCRs的当代观点及其信号转导复杂性的最新信息,并综述“经典”GPCRs在心血管生理学和疾病中的作用。然后,我们深入探讨了在心脏中研究较少的其他GPCRs,包括孤儿受体、嗅觉受体和味觉受体。我们认为,这些新型心脏GPCRs在健康和疾病状态下对心脏功能均有贡献,从而为通过治疗调节心脏功能提供了令人兴奋的机会。