protein
Apelin receptor
Gene
APLNR
Organism
Homo sapiens(9606)
Length
380 aa
Mass
42,660 Da
Apelin receptor (APLNR) is a G protein-coupled receptor that binds the peptide hormones apelin and apelin receptor early endogenous ligand (APELA), activating intracellular signaling pathways including Gi protein and beta-arrestin cascades (UniProt: P35414). The receptor regulates cardiovascular function, fluid homeostasis, angiogenesis, and heart morphogenesis during development and in adult physiology. In an alternative capacity, it serves as a coreceptor for HIV-1 entry and has been implicated in AIDS dementia pathogenesis (UniProt: P35414).
APLNR is expressed in cardiovascular and neural tissues, with established roles in vascular development, blood pressure regulation, and cardiac contractility. The receptor also functions as a mechanoreceptor responsive to pathological stimuli, though ligand-binding can suppress maladaptive cardiac hypertrophic responses.
In Alzheimer's Disease, APLNR is significantly upregulated in post-mortem AD brain tissue relative to age-matched controls (mean log2 fold-change: 1.50, Chaparral AD proteomics). The upregulation was detected across subcellular fractions in human TMT-labeled proteomics data, suggesting potential involvement in AD-related pathophysiology, though the functional consequence remains to be determined.
Generated from the curated entity record below. May contain errors — verify against source links.
Proteomics Evidence · AD
↑ Up in ADP3
not detected
P2
not detected
S2
not detected
S3
+1.500
Mean log₂FC across detected fractions: +1.4998 (1 of 4 fractions detected)
Human post-mortem AD brain vs age-matched controls, TMT-labeled, 4 subcellular fractions (P2, P3, S2, S3), DDA proteomics.
Related Publications
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Dujardin Simon et al.Nature medicine2020PMID 32572268Deep Multilayer Brain Proteomics Identifies Molecular Networks in Alzheimer's Disease Progression.
Bai Bing et al.Neuron2020PMID 31926610A Multi-network Approach Identifies Protein-Specific Co-expression in Asymptomatic and Symptomatic Alzheimer's Disease.
Seyfried Nicholas T et al.Cell systems2017PMID 27989508Large-scale deep multi-layer analysis of Alzheimer's disease brain reveals strong proteomic disease-related changes not observed at the RNA level.
Johnson Erik C B et al.Nature neuroscience2022PMID 35115731Organization and regulation of gene transcription.
Cramer PatrickNature2019PMID 31462772
Function
G protein-coupled receptor for peptide hormones apelin (APLN) and apelin receptor early endogenous ligand (APELA/ELA), that plays a role in the regulation of normal cardiovascular function and fluid homeostasis (PubMed:11090199, PubMed:22810587, PubMed:25639753, PubMed:28137936, PubMed:35817871, PubMed:38428423). When acting as apelin receptor, activates both G(i) protein pathway that inhibits adenylate cyclase activity, and the beta-arrestin pathway that promotes internalization of the receptor (PubMed:11090199, PubMed:25639753, PubMed:28137936, PubMed:35817871, PubMed:38428423). APLNR/APJ also functions as mechanoreceptor that is activated by pathological stimuli in a G-protein-independent fashion to induce beta-arrestin signaling, hence eliciting cardiac hypertrophy (PubMed:22810587, PubMed:38428423). However, the presence of apelin ligand blunts cardiac hypertrophic induction from APLNR/APJ on response to pathological stimuli (PubMed:22810587, PubMed:38428423). Plays a key role in early development such as gastrulation, blood vessels formation and heart morphogenesis by acting as a APELA receptor (By similarity). May promote angioblast migration toward the embryonic midline, i.e. the position of the future vessel formation, during vasculogenesis (By similarity). Promotes sinus venosus (SV)-derived endothelial cells migration into the developing heart to promote coronary blood vessel development (By similarity). Also plays a role in various processes in adults such as regulation of blood vessel formation, blood pressure, heart contractility and heart failure (PubMed:25639753, PubMed:28137936)
(Microbial infection) Alternative coreceptor with CD4 for HIV-1 infection; may be involved in the development of AIDS dementia (PubMed:11090199)
Sources
Last updated 5/8/2026, 6:31:37 AM