Journal
CURRENT DRUG TARGETS
Volume 16, Issue 2, Pages 148-155Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1389450115666141128120053
Keywords
Agonists; antagonists; anti-hypertension; apelin; APJ; novel compounds; target
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Funding
- National Natural Science Foundation of China [81270420, 81470434]
- Hengyang Joint Funds of Hunan Provincial Natural Science Foundation of China [12JJ8013]
- Hunan Provincial Natural Science Foundation of China [14JJ3102]
- Construct Program of the Key Discipline in Hunan Province
- Hunan Province Cooperative innovation Center for Molecular Target New Drug Study [Hunan Provincial Education Department document [2014-405]
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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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