Property Summary

NCBI Gene PubMed Count 64
Grant Count 80
R01 Count 29
Funding $23,168,322.94
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 0.000
colon cancer 1.800 0.000
interstitial cystitis 1.900 0.001
adult high grade glioma 1.300 0.027
pilocytic astrocytoma 1.600 0.002
sonic hedgehog group medulloblastoma -1.500 0.005
Pick disease 1.600 0.043
ovarian cancer 1.400 0.000

Synonym

Accession P35414
Symbols APJ
APJR
HG11
AGTRL1

Gene

PANTHER Protein Class (2)

PDB

2LOT   2LOU   2LOV   2LOW  

  TechDev Info (1)

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 (59)

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.
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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.
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