Property Summary

NCBI Gene PubMed Count 64
PubMed Score 238.94
PubTator Score 136.65

Knowledge Summary

Patent (20,816)

Expression

  Differential Expression (8)

Disease log2 FC p
posterior fossa group A ependymoma 3.200 1.8e-14
colon cancer 1.800 4.7e-04
interstitial cystitis 1.900 1.5e-03
adult high grade glioma 1.300 2.7e-02
pilocytic astrocytoma 1.600 2.0e-03
sonic hedgehog group medulloblastoma -1.500 5.0e-03
Pick disease 1.600 4.3e-02
ovarian cancer 1.400 7.1e-10

 CSPA Cell Line (2)

Protein-protein Interaction (286)

GNAT3   GRM8   CORT   CXCR6   CCL21   CXCL11   GRM6   CCL25   CCL16   ADCY6   GALR2   CXCL13   ADCY3   ADCY9   GALR3   GABBR2   S1PR2   ADCY5   S1PR4   C3   C5   KNG1   POMC   PENK   PDYN   PPY   NPY   PPBP   PF4   CXCL10   GNAI2   APP   GNAI3   CXCL1   SAA1   ADORA3   PYY   CXCL8   CCL5   DRD2   ADRA2C   GNAZ   CXCL2   CXCL3   PMCH   S1PR1   FPR1   CNR1   C5AR1   DRD4   GAL   CXCR1   CXCR2   FPR3   FPR2   ACKR3   NPY1R   BDKRB2   SSTR1   SSTR2   SSTR4   CCR1   CCR7   CXCR5   SSTR3   CNR2   SSTR5   OPRM1   DRD3   ADCY8   OPRD1   OPRK1   OPRL1   CASR   CCR2   CXCL5   PTGER3   CCR10   BDKRB1   GALR1   MTNR1A   CXCL12   NPBWR1   NPBWR2   NMU   PIK3CG   HCAR3   NPY2R   MTNR1B   CXCR3   NPY4R   P2RY4   CCR3   CCR4   CCR5   CCR6   CCR8   CCR9   ADCY7   CCL23   TAS2R38   TAS2R39   TAS2R40   TAS2R41   TAS2R43   TAS2R31   TAS2R45   TAS2R46   TAS2R30   TAS2R19   TAS2R20   TAS2R50   TAS2R60   GNG2   CXCR4   SST   GNB1   GNAI1   CCL20   CXCL6   PLCB2   PLCB3   GNA12   CXCL9   ADCY2   ADCY1   GPR17   PNOC   GPR18   GNA13   GRM2   GRM7   GRM3   GRM4   P2RY14   NPY5R   C3AR1   NMS   PIK3R6   TAS2R42   MT-RNR2   NPW   ADCY4   NPB   HCAR2   OXER1   RXFP4   RLN3   PIK3R5   LPAR1   ARHGEF1   MCHR2   OXGR1   S1PR3   GPER1   MCHR1   CCL19   P2RY13   SUCNR1   HCAR1   NMUR2   LPAR5   S1PR5   P2RY12   CXCL16   HRH4   NMUR1   LPAR2   PLCB1   CCL28   HEBP1   RXFP3   TAS2R16   TAS2R14   TAS2R13   TAS2R10   TAS2R9   TAS2R8   TAS2R7   TAS2R5   TAS2R4   TAS2R3   TAS2R1   ARHGEF12   GABBR1   LPAR3   GPR55   CCL27   HRH3   INSL5   PTGDR2   BTAF1   MDN1   TTI2   EXOC2   COQ8B   XPO1   ALG8   HIP1R   PDK1   EXOC4   INTS12   ARV1   SLC4A2   EXOC1   INTS2   ATP2B4   PDXDC1   FASTKD1   XPO7   BRAT1   ABHD17A   ABHD17B   GNL3L   GK   SLC29A1   ELOVL5   DNAAF5   PDS5B   RINT1   JAK1   IPO11   TTK   CPT2   SLC33A1   KIAA0368   THADA   SLC25A24   ADCK1   EXOC6   BDH1   OGG1   MCUB   COG2   TUBB3   SPG7   PDS5A   UFL1   NUS1   PTPN1   ATM   FANCA   MZT2B   SLC5A3   HACD2   SFXN5   EBP   SLC25A23   ARF5   DEGS1   DPY19L1   AGPAT5   ABHD18   XPR1   MTX1   INTS1   CHPT1   TMEM126B   NDC1   MTX3   MCU   AKR1D1   DAGLB   RAB3B   ZDHHC9   TMEM161B   GLMN   TUBGCP4   TUBGCP3   ATL3   MFSD9   NR2F6   NR2F2   AGPAT2   METTL15   ORC5   TMEM164   MT-CO1   SLC25A46   ABCD1   EDA   PEX16   ACAD10   C19orf25   MT-ND1   DOLK  

MLP Assay (20)

AID Type Active / Inconclusive / Inactive Description
2520 screening 347 / 0 / 330089 uHTS identification of small molecule agonists of the APJ receptor via a luminescent beta-arrestin assay
2521 screening 1062 / 0 / 329418 uHTS identification of small molecule antagonists of the APJ receptor via a luminescent beta-arrestin assay
2569 summary 0 / 0 / 0 Summary assay for small molecule antagonists of the APJ receptor
2580 summary 1 / 0 / 0 Summary assay for small molecule agonists of the APJ receptor
2764 screening 40 / 0 / 271 Single concentration confirmation of uHTS hits from a small molecule agonists of the APJ receptor via a luminescent beta-arrestin assay
2766 screening 622 / 0 / 326 Single concentration confirmation of uHTS hits from a small molecule antagonists of the APJ receptor via a luminescent beta-arrestin assay
2784 confirmatory 214 / 0 / 171 Dose Response confirmation of uHTS hits from a small molecule antagonists of the APJ receptor via a luminescent beta-arrestin assay
463109 confirmatory 25 / 0 / 31 SAR analysis of small molecule antagonists of the APJ receptor via a luminescent beta-arrestin assay
488748 confirmatory 2 / 0 / 75 Dose Response confirmation of uHTS hits from a small molecule agonists of the APJ receptor via a luminescent beta-arrestin assay
488803 confirmatory 16 / 0 / 93 SAR analysis of small molecule antagonists of the APJ receptor via a luminescent beta-arrestin assay - Set 2
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Gene RIF (58)

PMID Text
26676468 These findings suggested that Apelin/APLNR signaling may be used as a potential therapeutic target for hypoxic/ischemic injury.
26436483 The expressions of apelin and APJ are significantly augmented by hypoxia through the hypoxia-inducible factor-1 alpha (HIF-1alpha) signaling pathway.
25920569 apelin is produced by arterial endothelial cells (ECs) during embryogenesis, induces chemotaxis of venous ECs, and promotes the production of secreted Frizzled-related protein 1 by apelin receptor(+) ECs
25795508 Apelin-APJ system is a novel neurohormonal pathway, with studies to date suggesting that it may be of pathophysiologic relevance in Heart failure.
25359495 built 3 homology 3-D models of the ApelinR and revealed the conservation at the bottom of the apelin binding site of a hydrophobic cavity in which the C-terminal Phe of pE13F was embedded
25275559 This minireview outlines key (patho)physiological actions of the AR, addresses what is known about signal transduction downstream of AR activation
25275024 Apelin-APJ is overexpressed, and works as a signal for arteriogenesis in HCC.
25271156 serine 348 on the apelin receptor is a novel regulatory phosphorylation site in apelin-13-induced G protein-independent biased signaling
25184296 There was a significant correlation between APJ expression in myocardium resected after 10 min with both oxygen extraction ratio and mixed venous oxygen saturation in children undergoing surgical repair.
25062690 ERG and APLNR are essential for endothelial homeostasis in venules in the lung and that perturbation in ERG-APLNR signaling is crucial for the development of pulmonary veno-occlusive disease.
25060841 obese (especially diabese) youngsters demonstrated lower serum apelin levels; the G212A polymorphism of the APLNR gene was found to exert a favourable effect on circulating apelin levels in childhood obesity
24686079 APJ and B1R can form heterodimers in transfected HEK293 cells and activations of APJ and B1R could up-regulate eNOS phosphorylation
24465893 AGTRL1 genetic polymorphisms might contribute to the development of hypertension independently and/or through complex interaction.
24055369 REVIEW: Growing evidence shows that apelin/APJ system functions as a critical mediator of cardiovascular homeostasis and is involved in the pathophysiology of cardiovascular diseases.
23844873 functional role of the apelin--APJ system likely in early gestation
23438363 Introduce a new correlative NMR spectroscopy and computational biochemistry methodology and demonstrate its utility in providing some of the first high-resolution structural information for a peptide-activated apelin receptor transmembrane domain.
23226564 Interactive effects of genetic defects in apelin/APJ pathway might confer a potential risk in Chinese hypertensive patients.
22995518 Apelin/APJ pathway serves as a critical intermediary that links statin to its pleiotropic effects in regulating endothelial gene targets and function.
22842622 APJ, a seven transmembrane domain G-protein-coupled receptor, functions as a coreceptor for gp120 from some HIV-1 strains; a natural peptide ligand for APJ, apelin-13, efficiently blocks APJ coreceptor activity
22611158 APELIN promotes hematopoiesis from human embryonic stem cells.
22112232 Apelin may be associated with proliferative vasculopathy in systemic sclerosis.
22109355 There was an increased frequency of the G212 allele of AJP receptor in patients with hypertension in respect to patients without hypertension.
22037214 the novel peptide apelin and its receptor APJ can induce the morphological and functional maturation of blood vessels in tumors
21450694 hypoxia and inflammatory factors could play a major role in the activation of the hepatic apelin system leading to angiogenic and fibroproliferative response occurring in chronic liver disease.
21412239 demonstrated that non-activated APJ may suppress Ang II-AT(1) signaling, whereas this ligand-independent function was diminished with apelin activation
21233449 Disruption of apelin-APJ signaling can exacerbate pulmonary hypertension mediated by decreased activation of AMP-activated kinase and eNOS.
20921899 APJ, a seven transmembrane domain G-protein-coupled receptor, functions as a coreceptor for gp120 from some HIV-1 strains; a natural peptide ligand for APJ, apelin-13, efficiently blocks APJ coreceptor activity
20675385 These findings bring new insights into apelin receptor activation and show that Phe(255) and Trp(259), by interacting with the C-terminal Phe of the pyroglutamyl form of apelin 13 (pE13F) or K17F, are crucial for apelin receptor internalization.
20485192 found robust haplotype-based and haplotype-phenotype associations of four well characterized polymorphisms in apelin-AGTRL1 system with hypertension and related phenotypes
20353754 These observations revealed a novel ligand-dependent targeting of the apelin receptor to beta-arrestin-associated and -dissociated trafficking pathways and a role for different Rab proteins to direct these pathways.
20224560 Our study indicates that genetic variation of APLN-APJ and ACE2 may influence BP response to potassium intake.
20224560 Observational study of gene-disease association. (HuGE Navigator)
20220056 The apelin/APJ system may be involved in retinal neovascularization during the development of proliferative diabetic retinopathy.
20125035 Single nucleotide polymorphisms of the APLNR gene were significantly associated with diastolic blood pressure and mean arterial blood pressure responses to low-sodium intervention.
20099713 Aortic valve stenosis is characterized by an up-regulation of the apelin-APJ signaling pathway.
20055692 While apelin/APJ myocardial expression decreases, apelin plasma levels increase in left ventricular hypertrophy
19926159 No association between APLNR mRNA expression and gestational diabetes.
19680269 AGTRL1 polymorphism is not associated with coronary artery disease.
19680269 Observational study of gene-disease association. (HuGE Navigator)
19527631 Endothelial expression of apelin receptors is observed during the embryonic formation of blood vessels. The apelin system is both involved in physiological angiogenesis and pathological neoangiogenesis. Review.
19307984 genetic variation within apelin and AGTRL1 likely contributes to essential hypertension, BMI and the onset age of hypertension
19307984 Observational study of gene-disease association. (HuGE Navigator)
19123778 Nuclear magnetic resonance and circular dichroism spectroscopy results are presented for a variety of apelin peptides at both physiological and low temperatures allowing determination of the bioactive structure of apelin.
19069168 Observational study and genome-wide association study of gene-disease association. (HuGE Navigator)
18401529 In conclusion, the ERK1/2, but not p38 MAPK pathway is activated by apelin-13 through coupling of human APJ to Gi2-protein, which contributes to cellular responses.
17826642 Observational study of gene-disease association. (HuGE Navigator)
17412318 Apelin and APJ expression is highly upregulated in microvascular proliferations of brain tumors such as malignant gliomas.
17309882 Observational study of gene-disease association. (HuGE Navigator)
17309882 The results indicate that the SNP in the AGTRL1 gene is associated with the susceptibility to brain infarction.
17128405 apelin and APJ are expressed in preeclamptic placentas and may have a role in development of preeclampsia
15664671 reported the presence of APJ receptor-like immunoreactivity on cardiomyocytes, vascular smooth muscle cells and endothelial cells and the presence of apelin-like immunoreactivity in secretory vesicles of vascular endothelial cells
15087458 APJ exerts the hypotensive effect in vivo and plays a counterregulatory role against the pressor action of angiotensin II
14675627 second 10 residues of the N-terminal domain of APJ are critical for association with apelin, while the first 20 amino acids play an important role in supporting cell-cell fusion mediated by HIV-1 gp120
14645236 results demonstrate that apelin receptor exhibits nuclear localization in brain, distinct cell-dependent mechanisms for the nuclear transport of apelin receptors, and disruption of nuclear signal sequence disrupts its nuclear translocation
12667811 internalization and recycling, in stably expressing indicator cells, human neurons, primary CNS microvascular endothelial cells, and astrocytes
11040134 APJ, a seven transmembrane domain G-protein-coupled receptor, functions as a coreceptor for gp120 from some HIV-1 strains; a natural peptide ligand for APJ, apelin-13, efficiently blocks APJ coreceptor activity
9736741 APJ, a seven transmembrane domain G-protein-coupled receptor, functions as a coreceptor for gp120 from some HIV-1 strains; a natural peptide ligand for APJ, apelin-13, efficiently blocks APJ coreceptor activity
9653051 APJ, a seven transmembrane domain G-protein-coupled receptor, functions as a coreceptor for gp120 from some HIV-1 strains; a natural peptide ligand for APJ, apelin-13, efficiently blocks APJ coreceptor activity

AA Sequence

MEEGGDFDNYYGADNQSECEYTDWKSSGALIPAIYMLVFLLGTTGNGLVLWTVFRSSREKRRSADIFIAS      1 - 70
LAVADLTFVVTLPLWATYTYRDYDWPFGTFFCKLSSYLIFVNMYASVFCLTGLSFDRYLAIVRPVANARL     71 - 140
RLRVSGAVATAVLWVLAALLAMPVMVLRTTGDLENTTKVQCYMDYSMVATVSSEWAWEVGLGVSSTTVGF    141 - 210
VVPFTIMLTCYFFIAQTIAGHFRKERIEGLRKRRRLLSIIVVLVVTFALCWMPYHLVKTLYMLGSLLHWP    211 - 280
CDFDLFLMNIFPYCTCISYVNSCLNPFLYAFFDPRFRQACTSMLCCGQSRCAGTSHSSSGEKSASYSSGH    281 - 350
SQGPGPNMGKGGEQMHEKSIPYSQETLVVD                                            351 - 380
//

Text Mined References (64)

PMID Year Title
26676468 2016 Hypoxia induces the proliferation of endothelial progenitor cells via upregulation of Apelin/APLNR/MAPK signaling.
26436483 2015 Apelin/APJ signaling in hypoxia-related diseases.
25920569 2015 APJ Regulates Parallel Alignment of Arteries and Veins in the Skin.
25795508 2015 The Emerging Potential of the Apelin-APJ System in Heart Failure.
25359495 2015 New structural insights into the apelin receptor: identification of key residues for apelin binding.
25275559 2014 The apelin receptor: physiology, pathology, cell signalling, and ligand modulation of a peptide-activated class A GPCR.
25275024 2014 The apelin-APJ system induces tumor arteriogenesis in hepatocellular carcinoma.
25271156 2014 Identification of serine 348 on the apelin receptor as a novel regulatory phosphorylation site in apelin-13-induced G protein-independent biased signaling.
25184296 2014 Apelin receptor (APJ) expression during cardiopulmonary bypass in children undergoing surgical repair.
25062690 2014 ERG-APLNR axis controls pulmonary venule endothelial proliferation in pulmonary veno-occlusive disease.
25060841 2015 Apelin and G212A apelin receptor gene polymorphism in obese and diabese youth.
24686079 2014 Heterodimerization of human apelin and bradykinin 1 receptors: novel signal transduction characteristics.
24465893 2014 The contributory role of angiotensin receptor-like 1 gene multiple polymorphisms in hypertension among northeastern Han Chinese.
24055369 2014 Apelin and its receptor APJ in cardiovascular diseases.
23844873 2013 Decreased expression of apelin in placentas from severe pre-eclampsia patients.
23438363 2013 Structural features of the apelin receptor N-terminal tail and first transmembrane segment implicated in ligand binding and receptor trafficking.
23226564 2012 Interactive association of five candidate polymorphisms in Apelin/APJ pathway with coronary artery disease among Chinese hypertensive patients.
22995518 2012 Apelin/APJ signaling is a critical regulator of statin effects in vascular endothelial cells--brief report.
22611158 2012 APELIN promotes hematopoiesis from human embryonic stem cells.
22112232 2013 Serum apelin levels: clinical association with vascular involvements in patients with systemic sclerosis.
22109355 2012 APJ polymorphisms in coronary artery disease patients with and without hypertension.
22037214 2012 The apelin/APJ system induces maturation of the tumor vasculature and improves the efficiency of immune therapy.
21450694 2011 Hypoxia and proinflammatory factors upregulate apelin receptor expression in human stellate cells and hepatocytes.
21412239 2011 Non-activated APJ suppresses the angiotensin II type 1 receptor, whereas apelin-activated APJ acts conversely.
21233449 2011 Disruption of the apelin-APJ system worsens hypoxia-induced pulmonary hypertension.
20675385 2010 By interacting with the C-terminal Phe of apelin, Phe255 and Trp259 in helix VI of the apelin receptor are critical for internalization.
20485192 2010 Validation of genetic association in apelin-AGTRL1 system with hypertension in a larger Han Chinese population.
20353754 2010 The fate of the internalized apelin receptor is determined by different isoforms of apelin mediating differential interaction with beta-arrestin.
20224560 2010 Association of genetic variants in the apelin-APJ system and ACE2 with blood pressure responses to potassium supplementation: the GenSalt study.
20220056 2010 Apelin in plasma and vitreous and in fibrovascular retinal membranes of patients with proliferative diabetic retinopathy.
20125035 2010 Genetic variants in the apelin system and blood pressure responses to dietary sodium interventions: a family-based association study.
20099713 2009 Apelin and its receptor APJ in human aortic valve stenosis.
20055692 2010 Correlation between plasma levels of apelin and myocardial hypertrophy in rats and humans: possible target for treatment?
19926159 2010 Plasma apelin levels and apelin/APJ mRNA expression in patients with gestational diabetes mellitus.
19680269 2009 Validation of the association between AGTRL1 polymorphism and coronary artery disease in the Japanese and Korean populations.
19527631 2009 [Apelin signalisation and vascular physiopathology].
19307984 2009 Family-based analysis of apelin and AGTRL1 gene polymorphisms with hypertension in Han Chinese.
19123778 2009 Structural insight into G-protein coupled receptor binding by apelin.
19069168 2008 [Genetic risk factors of ischemic stroke identified by a genome-wide association study].
18577758 2008 Dissociation of heterotrimeric g proteins in cells.
18401529 2008 Apelin-13 induces ERK1/2 but not p38 MAPK activation through coupling of the human apelin receptor to the Gi2 pathway.
18240029 2008 Reviews in molecular biology and biotechnology: transmembrane signaling by G protein-coupled receptors.
17826642 2007 The 212A variant of the APJ receptor gene for the endogenous inotrope apelin is associated with slower heart failure progression in idiopathic dilated cardiomyopathy.
17412318 2007 Paracrine and autocrine mechanisms of apelin signaling govern embryonic and tumor angiogenesis.
17309882 2007 Functional SNP in an Sp1-binding site of AGTRL1 gene is associated with susceptibility to brain infarction.
17128405 2007 Modulation of apelin and APJ receptor in normal and preeclampsia-complicated placentas.
16303743 2005 Signal sequence and keyword trap in silico for selection of full-length human cDNAs encoding secretion or membrane proteins from oligo-capped cDNA libraries.
15664671 2005 Immunocytochemical localisation of the apelin receptor, APJ, to human cardiomyocytes, vascular smooth muscle and endothelial cells.
15489334 2004 The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).
15087458 2004 Regulatory roles for APJ, a seven-transmembrane receptor related to angiotensin-type 1 receptor in blood pressure in vivo.
14702039 2004 Complete sequencing and characterization of 21,243 full-length human cDNAs.
14675627 2003 The N-terminal domain of APJ, a CNS-based coreceptor for HIV-1, is essential for its receptor function and coreceptor activity.
14645236 2004 Agonist-independent nuclear localization of the Apelin, angiotensin AT1, and bradykinin B2 receptors.
14622440 2003 APJ receptor mRNA expression in the rat hypothalamic paraventricular nucleus: regulation by stress and glucocorticoids.
12667811 2003 Cell-cell fusion and internalization of the CNS-based, HIV-1 co-receptor, APJ.
12603839 2003 Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin.
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
11250876 2001 [(125)I]-(Pyr(1))Apelin-13 is a novel radioligand for localizing the APJ orphan receptor in human and rat tissues with evidence for a vasoconstrictor role in man.
11004481 2000 Distribution of mRNA encoding B78/apj, the rat homologue of the human APJ receptor, and its endogenous ligand apelin in brain and peripheral tissues.
10737800 2000 Shotgun sequencing of the human transcriptome with ORF expressed sequence tags.
9792798 1998 Isolation and characterization of a novel endogenous peptide ligand for the human APJ receptor.
8971794 1996 Low stringency hybridization study of the dopamine D4 receptor revealed D4-like mRNA distribution of the orphan seven-transmembrane receptor, APJ, in human brain.
8889548 1996 Normalization and subtraction: two approaches to facilitate gene discovery.
8294032 1993 A human gene that shows identity with the gene encoding the angiotensin receptor is located on chromosome 11.