Kalea Anastasia Z, Batlle Daniel
Northwestern University, Feinberg School of Medicine, Division of Nephrology/Hypertension, 303 East Chicago Avenue, Tarry Building 4-750, Chicago, IL 60611-3008, USA.
Curr Opin Investig Drugs. 2010 Mar;11(3):273-82.
Apelin is a peptide that has been identified as the endogenous ligand for the receptor APJ. The apelin/APJ system may be an important factor in the regulation of vascular tone and cardiovascular function. Studies on cultured cells and small animal models have revealed that apelin and APJ are localized in cardiomyocytes and vascular cells. The infusion of apelin affects vascular tone and blood pressure, with both central and peripheral actions. In clinical conditions such as heart failure and atherosclerosis, the gene expression of APJ and apelin, as well as the levels of circulating apelin, may be altered. The only known active homolog of ACE, ACE2, hydrolyzes apelin with similar potency to angiotensin II and, therefore, is responsible for the degradation of both peptides. Emerging data on a potential interaction between the two pathways suggest that the function of apelin/APJ in the vasculature may be relevant to cardiovascular disease, and identifying how this system is regulated could be useful clinically.
阿片肽是一种已被鉴定为受体APJ内源性配体的肽。阿片肽/APJ系统可能是调节血管张力和心血管功能的重要因素。对培养细胞和小动物模型的研究表明,阿片肽和APJ定位于心肌细胞和血管细胞中。输注阿片肽会影响血管张力和血压,具有中枢和外周作用。在心力衰竭和动脉粥样硬化等临床病症中,APJ和阿片肽的基因表达以及循环阿片肽水平可能会发生改变。已知唯一与血管紧张素转换酶(ACE)有活性的同源物,即血管紧张素转换酶2(ACE2),以与血管紧张素II相似的效力水解阿片肽,因此负责这两种肽的降解。关于这两条途径之间潜在相互作用的新数据表明,阿片肽/APJ在脉管系统中的功能可能与心血管疾病相关,确定该系统如何被调节在临床上可能有用。