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ADORA3

Official Full Name
adenosine A3 receptor
Organism
Homo sapiens
GeneID
140
Background
This gene encodes a protein that belongs to the family of adenosine receptors, which are G-protein-coupled receptors that are involved in a variety of intracellular signaling pathways and physiological functions. The receptor encoded by this gene mediates a sustained cardioprotective function during cardiac ischemia, it is involved in the inhibition of neutrophil degranulation in neutrophil-mediated tissue injury, it has been implicated in both neuroprotective and neurodegenerative effects, and it may also mediate both cell proliferation and cell death. Alternative splicing results in multiple transcript variants. This gene shares its 5' terminal exon with some transcripts from overlapping GeneID:57413, which encodes an immunoglobulin domain-containing protein. [provided by RefSeq, Nov 2014]
Synonyms
A3AR;
Bio Chemical Class
GPCR rhodopsin
Protein Sequence
MPNNSTALSLANVTYITMEIFIGLCAIVGNVLVICVVKLNPSLQTTTFYFIVSLALADIAVGVLVMPLAIVVSLGITIHFYSCLFMTCLLLIFTHASIMSLLAIAVDRYLRVKLTVRYKRVTTHRRIWLALGLCWLVSFLVGLTPMFGWNMKLTSEYHRNVTFLSCQFVSVMRMDYMVYFSFLTWIFIPLVVMCAIYLDIFYIIRNKLSLNLSNSKETGAFYGREFKTAKSLFLVLFLFALSWLPLSIINCIIYFNGEVPQLVLYMGILLSHANSMMNPIVYAYKIKKFKETYLLILKACVVCHPSDSLDTSIEKNSE
Open
Disease
Cerebral ischaemia, Glaucoma, Heart failure, Hepatitis virus infection, Ischaemic heart disease, Ischaemic/haemorrhagic stroke, Ischemia, Liver cancer, Malaria, Multiple sclerosis, Postoperative inflammation, Psoriasis, Rheumatoid arthritis, Solid tumour/cancer
Approved Drug
0
Clinical Trial Drug
9 +
Discontinued Drug
4 +

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Detailed Information

Comprising seven transmembrane domains, an external N-terminus, and an intracellular C-terminus, ADORA3 is a member of the G-protein-coupled receptor superfamily. Consistent with human chromosome 1p13.2, the ADORA3 gene has two exons. Especially displaying many splice variants, ADORA3 may have diverse expression patterns and functions in different tissues, therefore complicating the control of ADORA3.

Figure 1 illustrates the signaling pathways mediated by A3 adenosine receptors (A3AR) that confer cardiovascular protective effects through various mechanisms involving Gαq and Gαi protein activation.Figure 1. A3AR-mediated signaling pathways for cardiovascular protective effects. (Duangrat R, et al., 2024)

Signal Transduction Pathways

ADORA3 mainly reduces adenylyl cyclase activity upon activation by Gi proteins, hence lowering intracellular cyclic adenosine monophosphate (cAMP) levels. In cardiomyocytes especially, this mechanism is crucial as the drop in cAMP levels might lower calcium influx, therefore shielding cardiomyocytes from ischemia-reperfusion damage.

Apart from the Gi protein-mediated signaling pathway, ADORA3 may also activate phospholipase C (PLC) via Gq proteins, therefore fostering inositol triphosphate (IP3) synthesis and release of intracellular calcium. Control of cell proliferation, differentiation, and survival depends on this mechanism. Moreover, ADORA3 helps to activate the extracellular regulated kinase (ERK) pathway, which is essential for cell survival and multiplication.

ADORA3 signaling is mostly influenced by ATP-sensitive potassium (KATP) channels. Opening of KATP channels resulting from ADORA3 activation is thought to be a fundamental mechanism underlying its cardioprotective actions during ischemia episodes. By adjusting membrane potential and cellular energy metabolism, the regulation of KATP channels by ADORA3 helps to provide vaso-protection and cardio-protection.

ADORA3 in Various Pathological Conditions

Because the adenosine A3 receptor (ADORA3) shows a wide spectrum of activities in many physiological systems, it is a topic of great interest in many diseases. Although its significance in cardiovascular illnesses has been well-documented, new studies point to the major involvement of ADORA3 in other disorders including hypertension, liver ailments, and inflammatory skin problems.

ADORA3 shows a multifarious involvement in the cardiovascular system, especially in terms of vascular flow and hypertension. Recent research indicates that ADORA3 is widely distributed in endothelial cells and vascular smooth muscle cells, implying a fundamental part in the pathophysiology of vascular disorders.

ADORA3 signaling has been linked in mouse models to vascular constriction. Using an ADORA3 agonist, Cl-IBMECA, contractions in wild-type mouse aorta with intact endothelium were produced but not in tissue deprived of endothelium. Abolition of this effect in ADORA3-knockout mice suggests direct involvement of the receptor in the control of vascular tone. Fascinatingly, contraction induced by ADORA3 mostly depended on the endothelial cyclooxygenase-1 (COX-1) signaling system.

Further research using ADORA3-knockout mice models revealed that reactive oxygen species (ROS) generation mediated by ADORA3 via the activation of nicotinamide adenine dinucleotide phosphate (NADPH) oxidase subtype 2 or NOX2 showed involvement of vascular contraction. These results imply possible consequences for the therapy of hypertension by stressing the complicated interaction between ADORA3 and vascular function.

Future Direction

The many activities of ADORA3 in different clinical states underline its potential therapeutic target in several disorders. The translational potential of ADORA3 agonists is much better shown by the clinical trials including namodenoson and piclidenoson. To completely grasp the function of the receptor in every scenario, however, the complicated and even conflicting results of ADORA3 activation need thorough study. Several important topics need further study as science advances:

1. clarifying in chronic disorders the long-term consequences of ADORA3 modification.

2. Appreciating the interaction of the receptor with many signaling channels.

3. Creating highly selective ADORA3 antagonists and agonists with ideal pharmacokinetic characteristics for various therapeutic uses.

4. Running bigger, more thorough clinical studies to prove across many disorders the safety and effectiveness of ADORA3-targeted treatments.

References:

  1. Federico S, Spalluto G. Therapeutic potential of A2 and A3 adenosine receptor: a review of novel patented ligands. Expert Opin Ther Pat. 2012;22(4):369-390.
  2. Duangrat R, Parichatikanond W, Chanmahasathien W, et al. Adenosine A3 Receptor: From Molecular Signaling to Therapeutic Strategies for Heart Diseases. Int J Mol Sci. 2024;25(11):5763.
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