PUBLICATION
The apelin receptor: physiology, pathology, cell signalling, and ligand modulation of a peptide-activated class A GPCR
- Authors
- Chapman, N.A., Dupré, D.J., Rainey, J.K.
- ID
- ZDB-PUB-141003-1
- Date
- 2014
- Source
- Biochemistry and cell biology = Biochimie et biologie cellulaire 92(6): 431-40 (Review)
- Registered Authors
- Keywords
- APJ, APLNR, RCPG activé par un peptide, apelinergic system, peptide-activated GPCR, signal transduction, système apelinergique, transduction de signal
- MeSH Terms
-
- Animals
- Cardiovascular Diseases/genetics
- Cardiovascular Diseases/metabolism
- Cardiovascular Diseases/pathology
- Diabetes Mellitus/genetics
- Diabetes Mellitus/metabolism
- Diabetes Mellitus/pathology
- Embryo, Nonmammalian/embryology
- Embryonic Development/genetics
- Humans
- Intercellular Signaling Peptides and Proteins/genetics
- Intercellular Signaling Peptides and Proteins/metabolism*
- Neoplasms/genetics
- Neoplasms/metabolism
- Neoplasms/pathology
- Obesity/genetics
- Obesity/metabolism
- Obesity/pathology
- Receptors, G-Protein-Coupled/genetics
- Receptors, G-Protein-Coupled/metabolism*
- Signal Transduction*
- Zebrafish/embryology
- Zebrafish/genetics
- Zebrafish Proteins/genetics
- Zebrafish Proteins/metabolism
- PubMed
- 25275559 Full text @ Biochem. Cell Biol.
Citation
Chapman, N.A., Dupré, D.J., Rainey, J.K. (2014) The apelin receptor: physiology, pathology, cell signalling, and ligand modulation of a peptide-activated class A GPCR. Biochemistry and cell biology = Biochimie et biologie cellulaire. 92(6):431-40.
Abstract
The apelin receptor (AR or APJ) is a class A (rhodopsin-like) G-protein-coupled receptor with wide distribution throughout the human body. Activation of the AR by its cognate peptide ligand, apelin, induces diverse physiological effects including vasoconstriction and dilation, strengthening of heart muscle contractility, angiogenesis, and regulation of energy metabolism and fluid homeostasis. Recently, another endogenous peptidic activator of the AR, Toddler/ELABELA, was identified as having a crucial role in zebrafish (Danio rerio) embryonic development. The AR is also implicated in pathologies including cardiovascular disease, diabetes, obesity, and cancer, making it a promising therapeutic target. Despite its established importance, the precise roles of AR signalling remain poorly understood. Moreover, little is known about the mechanisms of peptide-AR activation. Additional complexity arises from modulation of the AR by 2 endogenous peptide ligands, both with multiple bioactive isoforms of variable length and distribution. The various apelin and Toddler/ELABELA isoforms may also produce distinct cellular effects. Further complexity arises through formation of functionally distinct heterodimers between the AR and other G-protein-coupled receptors. This minireview outlines key (patho)physiological actions of the AR, addresses what is known about signal transduction downstream of AR activation, and concludes by discussing unique properties of the endogenous peptidic ligands of the AR.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping