Apelin, a regulatory peptide, is an endogenous ligand of the apelin receptor (APJ), which belongs to the G protein-coupled receptor family. The peptide and its receptor are distributed in animal and human tissues, including the cardiovascular and central nervous systems, and studies indicate that apelin signaling could play a role in cytoprotection of cells where it is found. Apelin activity may be modulated by interactions of the APJ receptor with other receptors that result in heteromerization. The interaction of the APJ with other receptor systems increases the signaling repertoire of apelin, thereby allowing it to exert a widened degree of control over cellular physiological functions. This article reviews studies which provide evidence for the physiological importance of APJ/Kappa opioid receptor (KOR) heterodimers in several critical cellular processes, including cell proliferation, and results are discussed that support a role of this peptide and the APJ receptor in functioning of the cardiovascular, gastrointestinal and central nervous systems under normal conditions and pathology, as well as novel signal transduction characteristics resulting following the interaction of APJ and KOR. A better understanding of the cellular protective actions of apelin, and the physiological outcomes from interaction of its receptor with other receptor types could lead to new pharmaceutical targets for various diseases affecting among other organs, the heart, the gastrointestinal system and the brain.
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http://dx.doi.org/10.1016/j.ejphar.2022.175353 | DOI Listing |
Anticancer Agents Med Chem
January 2025
Department of Pharmaceutical Sciences, Lucknow University, Lucknow, UP, India.
In women globally, breast cancer ranks as the second most frequent cause of cancer-related deaths, making up about 25% of female cancer cases, which is pretty standard in affluent countries. Breast cancer is divided into subtypes based on aggressive, genetic and stage. The precise cause of the problem is still unknown.
View Article and Find Full Text PDFJ Adv Res
December 2024
Department of Orthopaedics, The First Affiliated Hospital of Soochow University, 188 Shizi Street, Suzhou 215006, Jiangsu, China. Electronic address:
Introduction: Inflammatory diseases, such as diabetes mellitus, rheumatoid arthritis, and inflammatory bowel disease, lead to systemic immune microenvironment disturbances, contributing to bone loss, yet the mechanisms by which specific receptors regulate this process in inflammatory bone loss remain poorly understood. As a G-protein-coupled receptor, the Apelin receptor plays a crucial role in the regulation of inflammation and immune microenvironment. However, the precise mechanisms governing its role in inflammatory bone loss remain incompletely understood.
View Article and Find Full Text PDFNeuroscience
December 2024
Rehabilitation Sciences and Engineering, University of Health and Rehabilitation Sciences, Qingdao 266071, China. Electronic address:
Apelin, an endogenous ligand of G protein-coupled receptor APJ, is widely distributed in the central nervous system (CNS). It can be divided into such subtypes as Apelin-13, Apelin-17, and Apelin-36 as they have different amino acid structures. All Apelin is widely studied as an adipokine, showing a significant protective effect through regulating apoptosis, autophagy, oxidative stress, angiogenesis, inflammation, and other pathophysiological processes.
View Article and Find Full Text PDFBiomedicines
November 2024
Division of Medical Biology, Faculty of Nursing and Midwifery, Wroclaw Medical University, 50-368 Wrocław, Poland.
: SARS-CoV-2 enters cells primarily by binding to the angiotensin-converting enzyme 2 (ACE2) receptor, thereby blocking its physiological functions, affecting the apelinergic system, and inhibiting the cleavage of its peptides. The appropriate concentration of peptides in the apelinergic system influences the maintenance of homeostasis and protects against cardiovascular diseases. In our research, we determined the level of selected parameters of the apelinergic system-apelin (AP), elabela (ELA), and the apelin receptor (APJ)-in repeat blood donors.
View Article and Find Full Text PDFFood Funct
December 2024
School of Chemistry, Pharmacy and Pharmacology, University of East Anglia, Norwich Research Park, Norwich NR4 7TJ, UK.
Based on its anti-inflammatory and antioxidant properties, (DC) Stapf is commonly used in traditional and modern medicine to cure different diseases. The present study investigates the potential of organic extract as an anti-obesity drug in a HCHFD (high-carbohydrate, high-fat diet) model for obese rats. Its negative hypolipidemic effect has been confirmed through biochemical and histological methods.
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