title: Apelin/APJ system as a therapeutic target in diabetes and its complications.
abstract: The G-protein-coupled receptor APJ and its endogenous ligand apelin are widely expressed in many peripheral tissues and central nervous system, including adipose tissue, skeletal muscles and hypothalamus. Apelin/APJ system, involved in numerous physiological functions like angiogenesis, fluid homeostasis and energy metabolism regulation, is notably implicated in the development of different pathologies such as diabetes and its complications. Increasing evidence suggests that apelin regulates insulin sensitivity, stimulates glucose utilization and enhances brown adipogenesis in different tissues associated with diabetes. Moreover, apelin is also involved in the regulation of diabetic complications via binding to APJ receptor. Apelin improves diabetes-induced kidney hypertrophia, normalizes obesity-associated cardiac hypertrophy and negatively promotes retinal angiogenesis in diabetic retinopathy. In this review, we provide a comprehensive overview about the role of apelin/APJ system in different tissues related with diabetes. Furthermore, we describe the pathogenesis of diabetic complications associated with apelin/APJ system. Finally, agonists and antagonists targeted to APJ receptor are described in the literature. Thus, we highlight apelin/APJ system as a novel therapeutic target for pharmacological intervention in treating diabetes and its complications.
authors.affiliation: Institute of Pharmacy and Pharmacology, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China, Hengyang 421001, China.
authors.forename: Haoliang
authors.initials: H
authors.lastname: Hu
authors.affiliation: Institute of Pharmacy and Pharmacology, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China, Hengyang 421001, China; Department of Neurosurgery, The First Affiliated Hospital of University of South China, Hengyang 421001, China.
authors.forename: Lu
authors.initials: L
authors.lastname: He
authors.affiliation: Institute of Pharmacy and Pharmacology, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China, Hengyang 421001, China. Electronic address: llanfang6@126.com.
authors.forename: Lanfang
authors.initials: L
authors.lastname: Li
authors.affiliation: Institute of Pharmacy and Pharmacology, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China, Hengyang 421001, China. Electronic address: lxchen6@126.com.
authors.forename: Linxi
authors.initials: L
authors.lastname: Chen
mesh_terms: D000273:Adipose Tissue / Q000378:metabolism; D000073861:Apelin / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics*; D000075244:Apelin Receptors / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics*; D048909:Diabetes Complications / Q000188:drug therapy / Q000235:genetics* / Q000503:physiopathology; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy / Q000235:genetics* / Q000503:physiopathology; D004734:Energy Metabolism / Q000235:genetics; D005947:Glucose / Q000378:metabolism; D006706:Homeostasis; D006801:Humans; D007333:Insulin Resistance / Q000235:genetics; D008024:Ligands; D009765:Obesity / Q000188:drug therapy / Q000235:genetics* / Q000503:physiopathology; D011485:Protein Binding
chemical_list: C104575:APLNR protein, human; D000073861:Apelin; D000075244:Apelin Receptors; D008024:Ligands; D005947:Glucose
keywords: APJ; Apelin; Cardiopathy; Diabetes; ELABELA; Insulin resistance; Nephropathy; Obesity; Retinopathy