4.7 Article

Targeting the apelin pathway as a novel therapeutic approach for cardiovascular diseases

期刊

出版社

ELSEVIER SCIENCE BV
DOI: 10.1016/j.bbadis.2016.11.007

关键词

Apelin; Apelin receptor; Heart failure; Vascular disease; Apelin analogue

资金

  1. National Basic Research Program of China [2014CB542300]
  2. National Major Research Plan Training Program [91339108]
  3. National Natural Science Foundation of China [81370362, 81170246]
  4. Shanghai Municipal Education Commission-Gaofeng Clinical Medicine Grant [20152509]
  5. Canadian Institutes of Health Research (CIHR)
  6. Alberta Innovates-Health Solutions (AI-HS)

向作者/读者索取更多资源

The apelin/apelin receptor system is widely distributed and has a dominant role in cardiovascular homeostasis and disease. The apelin gene is X-linked and is synthesized as a 77 amino acid pre-pro-peptide that is subsequently cleaved to generate a family of apelin peptides that possess similar functions but display different tissue distribution, potency and receptor binding affinity. Loss-of-function experiments using the apelin and the apelin receptor knockout mice and gain-of-function experiments using apelin peptides have delineated a well-defined role of the apelin axis in cardiovascular physiology and diseases. Activation of the apelin receptor by its cognate peptide ligand, apelin, induces a wide range of physiological effects, including vasodilation, increased myocardial contractility, angiogenesis, and balanced energy metabolism and fluid homeostasis. The apelin/apelin receptor pathway is also implicated in atherosclerosis, hypertension, coronary artery disease, heart failure, diabetes and obesity, making it a promising therapeutic target. Hence, research is expanding to develop novel therapies that inhibit degradation of endogenous apelin peptides or their analogues. Chemical synthesis of stable apelin receptor agonists aims to more efficiently enhance the activation of the apelin system. Targeting the apelin/apelin receptor axis has emerged as a novel therapeutic approach against cardiovascular diseases and an increased understanding of cardiovascular actions of the apelin system will help to develop effective interventions. (C) 2016 Elsevier B.V. All rights reserved.

作者

我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。

评论

主要评分

4.7
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

暂无数据
暂无数据