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Symbol APLNR contributors: mct/npt - updated : 24-03-2020
HGNC name apelin receptor
HGNC id 339
  • seven transmembrane segments (7TM) receptor
  • C terminus of the APLNR also possesses multiple serine and threonine residues, which are potential sites of phosphorylation by GRK
  • mono polymer heteromer , dimer
  • G-protein coupled receptor 1 family
  • CATEGORY receptor membrane G
    SUBCELLULAR LOCALIZATION     plasma membrane
    basic FUNCTION
  • stimulating a phosphotyrosine phosphatase which inhibits guanylate cyclase
  • having a physiological role in mechanisms of water intake and fluid retention and suggest an anti-diuretic effect of apelin (Roberts 2009)
  • APLN/APLNR system functions as a critical mediator of cardiovascular homeostasis and is involved in the pathophysiology of cardiovascular diseases.
  • BDKRB1, APLNR are involved in a variety of important physiological processes, which share many similar characteristics in distribution and functions in the cardiovascular system
  • APLN/APLNR axis is involved in hypoxia-induced proliferation of Endothelial progenitor cells (EPCs)
  • plays a prominent role in the cardiomyocyte adapting to hypertrophic stimulation
  • APLN and APLNR may play a role in human follicular development and the pathogenesis of polycystic ovary syndrome (PCOS)
  • APELA-APLNR axis protects from pressure overload-induced heart failure possibly via suppression of ACE expression and pathogenic angiotensin II signalling
  • spinal apelin&
  • 8209;APLNR system may drive neuropathic pain
  • apelin/APLNR system plays a pivotal role in mediating the function of Vascular smooth muscle cell (VSMC)
  • plays an important role in aging
  • appears to be involved in regulation of renin-angiotensin-aldosterone system (RAAS), apoptosis, inflammation and oxidative stress which promotes aging
  • system plays diversified functions and regulatory roles in digestive physiology and pathology
  • APLNR signaling could be a migration related regulatory mechanism in cancer and wound healing
  • essential gene for cancer immunotherapy
  • induces vasodilation and vasoconstriction in blood vessels(
  • AGTR1 and APLNR are mechanosensitive GPCRs in the heart, playing vital roles in cardiac physiological adaptation to changes in mechanical load
  • APELA-APLNR axis is essential for diverse biological processes and has been shown to regulate fluid homeostasis, myocardial contractility, vasodilation, angiogenesis, cellular differentiation, apoptosis, oxidative stress, cardiorenal fibrosis, and dysfunction
    a component
  • AGTR1–APLNR heterodimers activate distinct signaling pathways compared to monomeric receptors, or the multiple reported downstream pathways of AGTR1 and APLNR may be partially dependent on the activation of the heterodimeric receptor
    small molecule
  • receptor of apelin (APLN), apelin-AGTRL1 signaling pathway emerges as an important novel mediator of cardiovascular control
  • APLN, APLNR signaling is a potent regulator of endothelial MEF2C function in the developing cardiovascular system
  • APLNR controls a regulatory CER1-SMARCD3 pathway in pluripotent stem cell cardiomyogenesis
  • is a key regulator of cardiovascular function and is activated by two different endogenous peptide ligands, APLN and APELA, each with different isoforms diversified by length and amino acid sequence
  • APLNR-enhanced response requires ADRA1A to contract vessels coordinately
  • cell & other
    Other regulated in a tissue-dependent manner and according to the severity of insulin resistance (Dray 2010)
    corresponding disease(s)
    Other morbid association(s)
    TypeGene ModificationChromosome rearrangementProtein expressionProtein Function
    constitutional     --over  
    in aortic valve stenosis, of the apelin-APLNR signaling pathway (Peltonen 2009)
    constitutional     --low  
    with increasing age
    constitutional       loss of function
    confers resistance to chronic pressure overload by markedly reducing myocardial hypertrophy and heart failure
    Susceptibility to brain infarction
    Variant & Polymorphism SNP SNP in the 5'-flanking region (SNP30, rs9943582, 154G/A) is significantly associated with brain infarction
    Candidate gene
  • APLNR expression in tumour vasculature and tumour cells is an independent prognostic factor for survival of patients with clear-cell Renal cell carcinoma
  • Therapy target
  • apelin-APLNR signaling pathway, is a possible novel target for drug discovery in calcified aortic valve disease by suppressing chemotaxis, angiogenesis and osteoblast activity, all of which are well-documented phenomena in the disease process (Peltonen 2009)
  • APELIN/APLNR system might become a novel promising therapeutic target for anti-aging
  • SystemTypeDisorderPubmed
    promising potential as a therapeutic target for treatment of neuropathy
    promising potential as a therapeutic target for treatment of psychosis
    apelin/APLNR system is a promising target for managing vascular disease
    may provide novel pharmacological interventions for neuropathic pain
    cardiovascularaquiredheart failure
    important therapeutic target for the treatment of heart failure, hypertension