Recombinant Human Protein ADORA3, isoform 3 (ADORA3)
Description
Introduction to Recombinant Human Protein ADORA3, Isoform 3
The Recombinant Human Protein ADORA3, isoform 3, refers to a specific variant of the adenosine A3 receptor, which is a G-protein-coupled receptor (GPCR) encoded by the ADORA3 gene in humans. This receptor plays a crucial role in various physiological processes, including anti-inflammatory, anticancer, and anti-ischemic effects, making it a promising therapeutic target for several diseases.
Structure and Function of ADORA3
The ADORA3 gene encodes a protein consisting of 318 amino acids, with seven transmembrane domains typical of GPCRs . The receptor is involved in signaling pathways that modulate the activity of adenylyl cyclase, phospholipase C, and intracellular calcium levels through its coupling with Gi and Gq proteins . The C-terminal segment contains numerous serine and threonine residues, which are potential sites for phosphorylation and desensitization of the receptor .
Therapeutic Potential of ADORA3
The adenosine A3 receptor is overexpressed in various neoplastic cells and inflammatory conditions, suggesting its potential as a therapeutic target . Highly selective A3AR agonists have been developed to exploit this overexpression for treating diseases such as rheumatoid arthritis, psoriasis, and certain cancers . These agonists modulate the Wnt and NF-κB signaling pathways to exert anti-inflammatory and anticancer effects .
Research Findings and Applications
Recent studies have identified novel ligands for the A3 receptor, such as N6-methyladenosine (m6A) and N6-isopentenyl adenosine (i6A), which exhibit selective agonist activity . The structural insights into the receptor's selectivity highlight the importance of hydrophobic residues in the binding pocket for agonist potency . Additionally, A3AR agonists have shown cardioprotective effects by reducing infarct size in models of ischemia/reperfusion injury .
Table 1: Expression and Therapeutic Targets of ADORA3
| Disease/Condition | Expression Level | Therapeutic Potential |
|---|---|---|
| Cancer (e.g., leukemia, melanoma) | High | Anticancer effects via modulation of signaling pathways |
| Inflammatory diseases (e.g., rheumatoid arthritis) | High | Anti-inflammatory effects through NF-κB and Wnt pathways |
| Ischemic conditions (e.g., heart ischemia) | Variable | Cardioprotective effects by reducing infarct size |
Table 2: Signaling Pathways Involved in ADORA3 Activation
| Pathway | Effect |
|---|---|
| Gi-coupled inhibition of adenylyl cyclase | Decrease in cAMP levels |
| Gq-coupled activation of phospholipase C | Increase in intracellular calcium |
| NF-κB signaling | Modulation of inflammatory responses |
| Wnt signaling | Regulation of cell proliferation and differentiation |
Product Specs
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