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APLNR

Official Full Name
apelin receptor
Organism
Homo sapiens
GeneID
187
Background
This gene encodes a member of the G protein-coupled receptor gene family. The encoded protein is related to the angiotensin receptor, but is actually an apelin receptor that inhibits adenylate cyclase activity and plays a counter-regulatory role against the pressure action of angiotensin II by exerting hypertensive effect. It functions in the cardiovascular and central nervous systems, in glucose metabolism, in embryonic and tumor angiogenesis and as a human immunodeficiency virus (HIV-1) coreceptor. Two transcript variants resulting from alternative splicing have been identified. [provided by RefSeq, Jul 2009]
Synonyms
APJ; APJR; HG11; AGTRL1;
Protein Sequence
MEEGGDFDNYYGADNQSECEYTDWKSSGALIPAIYMLVFLLGTTGNGLVLWTVFRSSREKRRSADIFIASLAVADLTFVVTLPLWATYTYRDYDWPFGTFFCKLSSYLIFVNMYASVFCLTGLSFDRYLAIVRPVANARLRLRVSGAVATAVLWVLAALLAMPVMVLRTTGDLENTTKVQCYMDYSMVATVSSEWAWEVGLGVSSTTVGFVVPFTIMLTCYFFIAQTIAGHFRKERIEGLRKRRRLLSIIVVLVVTFALCWMPYHLVKTLYMLGSLLHWPCDFDLFLMNIFPYCTCISYVNSCLNPFLYAFFDPRFRQACTSMLCCGQSRCAGTSHSSSGEKSASYSSGHSQGPGPNMGKGGEQMHEKSIPYSQETLVVD
Open
Disease
Heart failure
Approved Drug
0
Clinical Trial Drug
1 +
Discontinued Drug
0

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Detailed Information

Encoding the Apelin Receptor (also known as APJ), the APLNR gene has become quite important in several physiological processes and pathological disorders. Emphasizing its relevance in cardiovascular control, neurological processes, and disease etiology, this thorough study explores the molecular properties, ligand interactions, physiological activities, and possible therapeutic effects of APLNR.

Molecular Characteristics and Structure

Found on chromosome 11q12.1, APLNR falls within the G protein-coupled receptor (GPCR) gene family. The gene generates a 380-amino acid protein with over 40% sequence similarity to the angiotensin II receptor (AT2R). APLNR does not bind angiotensin II despite this structural similarity, which results in its original designation as an orphan receptor upon discovery in 1993.

Comprising seven transmembrane α-helical segments characteristic of the r Rhodopsin-like receptor subfamily A3, the APLNR protein is a class A GPCR. Using a 17-residue synthetic analog, recent X-ray crystallography investigations have shed important light on its structure, hence improving our knowledge of ligand-receptor interactions.

Figure 1 describes the signaling pathways associated with APLNR activation, specifically illustrating the mechanisms by which the APLNR receptor transmits signals through different pathways.Figure 1. Signaling pathways associated with activation of APLNR. (Ivanov MN, et al., 2022)

Ligands and Signaling Pathways

Early endogenous ligands for APLNR are apelin and apelin receptor early endogenous ligands (APELA). Originally separated from bovine stomach extracts in 1998, apelin is produced from a 77-amino acid precursor protein (preproapelin) encoded by an X chromosome gene. Apelin-55, -36, -17, and -13 are among the numerous bioactive peptides produced from this precursor by proteolytic cleavage; each has unique tissue distribution, binding affinities, and functional characteristics.

Using its ligands, APLNR activation reduces adenylate cyclase activity and initiates many intracellular signaling pathways. Important pathways linked to APLNR activation consist of:

1. G protein-dependent pathways: Inhibition of cAMP production and activation of ERK1/2.
2. G protein-independent pathways: β-arrestin-mediated signaling.
3. PI3K/Akt pathway: Involved in cell survival and angiogenesis.
4. ERK pathway: Regulates cell proliferation and differentiation.

These diverse signaling mechanisms underpin the wide-ranging physiological effects of the APLNR system.

Expression and Distribution

The broad distribution of APLNR and its ligands is seen in mammalian central and peripheral neural systems. APLNR expression is very prominent in the brain's entorhinal cortex as well as in specialized areas of the cerebral cortex including the frontal, temporal, occipital, and piriform lobes. RT-PCR shows that, in the brain, apelin mRNA levels are often greater than APLNR mRNA.

Expression of both APLNR and apelin is seen in the dentate gyrus and hippocampal region; apelin shows more levels. Fascinatingly, APLNR expression has been seen in neurogenic niches including the subventricular zone along the lateral ventricles (SVZa) in monkeys, indicating a possible function in adult neurogenesis.

Particularly in the supraoptic nucleus (SON) and paraventricular nucleus, the hypothalamus is another important location of APLNR and apelin expression, therefore implicating the system in fluid balance control. Other brain areas displaying apelin system components include the preoptic area, cerebellum, pituitary, medulla, pons, and spinal cord. At the cellular level, APLNR is not expressed in microglia but rather in neurons, oligodendrocytes, and astrocytes. Apelin expression is mostly neural; astrocytes and microglia lack it.

Physiological Functions

APLNR's many physiological functions are explained by its broad dispersion of ligands and APLNR throughout different tissues and organ systems:

APLNR is vital for cardiovascular function. It controls blood pressure by acting as a counter-regulator against the pressure action of angiotensin II. Involved in cardiac contraction, the receptor may contribute to the advancement of heart failure. Furthermore, the APLNR system is linked to blood vessel growth and angiogenesis—both in adult tissues and during embryonic development.

APLNR and apelin expression in hypothalamus nuclei linked with fluid balance points to an osmoregulation function. The system could control antidiuretic hormone release, affecting water retention and blood volume.

Emerging data suggests a function for the APLNR system in glucose metabolism. It might have effects on glucose absorption and insulin sensitivity, implying possible consequences for metabolic diseases like diabetes.

Neurological Functions

APLNR participates in many central nervous system functions:

1. Expression in neurogenic niches points to a possible function in controlling new neuron generation in the adult brain.
2. Activation of APLNR has been linked in models of brain damage and neurodegenerative disorders to neuroprotection.
3. APLNR's presence in the pituitary and hypothalamus suggests a function in the control of hormone production.

Especially in gastrulation, blood vessel development, and heart morphogenesis, APLNR and its ligands are vital players in early development. During vasculogenesis, the receptor drives angioblast migration towards the embryonic midline and helps sinus venosus-derived endothelial cells migrate into the developing heart, hence promoting coronary blood vessel growth.

References:

  1. Ivanov MN, Stoyanov DS, Pavlov SP, et al. Distribution, Function, and Expression of the Apelinergic System in the Healthy and Diseased Mammalian Brain. Genes (Basel). 2022;13(11):2172.
  2. Lam YY, Chan CH, Geng L, et al. APLNR marks a cardiac progenitor derived with human induced pluripotent stem cells. Heliyon. 2023;9(7):e18243.
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