Target intelligence / Profile preview

Adenosine Receptor A3 (A3AR)

Target
A3AR
Molecular classification
G Protein-Coupled Receptor, Receptor
01

Overview

The adenosine A3 receptor (A3AR), also known as ADORA3, is a G protein-coupled receptor (GPCR) that binds adenosine. Activation leads to inhibition of adenylate cyclase and activation of phospholipase pathways. It is implicated in cardioprotection, immunomodulation, and neuroprotection/neurodegeneration. Overexpression in inflammatory and cancer cells makes it a target for anti-inflammatory and anticancer therapies. Clinical trials are ongoing with selective agonists for rheumatoid arthritis, and antagonists show potential for asthma treatment.

Other names
ADORA3
02

Mechanism of action

Gi/Gq protein coupling leading to inhibition of adenylate cyclase, activation of phospholipase Cβ (PLCβ), phospholipase D (PLD), PI3Kγ pathways, raising cytosolic Ca²⁺ concentration and activating PKC/ERK MAP kinases

03

Biological functions

Signal transductionImmunomodulationCardioprotectionNeuroprotectionNeurodegenerationRegulation of adenylate cyclase activityPhospholipase Cβ activationPhospholipase D activationPI3Kγ pathway activation
04

Disease associations

Cardiovascular diseaseInflammationCancerRheumatoid arthritisAsthma
05

Interacting drugs

CF101/Piclidenoson

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