摘要
APJ是一个类视紫红质 G 蛋白耦合受体(GPCR)与血管紧张素受体AT1高序列相似性。APJ已被证明是广泛表达于人类组织,包括中枢神经系统、心血管系统、组织和其他部位。APJ在心血管和代谢疾病包括动脉粥样硬化(AS)、冠心病(CAD)、心力衰竭(HF)、肺动脉高血压(PAH)、心肌肥大和房颤,特别是高血压的发生和发展中发挥着重要作用。先前的研究人员发现,apelin/APJ 能诱导血管舒张并降低血压。尽管APJ与许多疾病密切相关,但是没有药物可以直接激活或抑制APJ。在本综述中,我们总结了针对于APJ的肽、小分子受体激动剂和拮抗剂的最新报道。apelin /APJ在高血压和其他心血管疾病发挥了重要作用。我们相信开发基于APJ的肽和化合物可用于治疗这些疾病。
关键词: 受体激动剂,拮抗剂,降血压,内源性配体,APJ,新颖的化合物,靶点
Current Drug Targets
Title:Targeting Drugs to APJ Receptor: The Prospect of Treatment of Hypertension and Other Cardiovascular Diseases
Volume: 16 Issue: 2
Author(s): Jiangang Cao, Hening Li and Linxi Chen
Affiliation:
关键词: 受体激动剂,拮抗剂,降血压,内源性配体,APJ,新颖的化合物,靶点
摘要: The APJ is a class A, rhodopsin-like G protein-coupled receptor (GPCR) with high sequence similarity to the angiotensin receptor AT1. APJ has been shown to be widely expressed in humans tissues, including the central nervous system, cardiovascular system, adipocytes and others. APJ plays an important role in the occurrence and development of cardiovascular and metabolic diseases including atherosclerosis (AS), coronary heart disease (CAD), heart failure(HF), pulmonary arterial hypertension (PAH), myocardial hypertrophy and atrial fibrillation, especially hypertension. Previous researchers found that apelin/APJ could induce vasodilation and then reduce blood pressure. Despite APJ is closely associated with many diseases, there are no drugs that can activate or inhibit APJ directly. In the current review, we have summarized recently reported peptides, small molecule agonists and antagonists targeting APJ. Given the role of apelin/APJ in hypertension and other cardiovascular diseases, we believe that the peptides and compounds based on APJ will be developed for treatment of these diseases.
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Jiangang Cao, Hening Li and Linxi Chen , Targeting Drugs to APJ Receptor: The Prospect of Treatment of Hypertension and Other Cardiovascular Diseases, Current Drug Targets 2015; 16 (2) . https://dx.doi.org/10.2174/1389450115666141128120053
DOI https://dx.doi.org/10.2174/1389450115666141128120053 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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