A2A Adenosine receptors are powerful therapeutic targets especially found in the treatment of such conditions as insomnia, pain, depression, and Parkinson’s disease.
This class A GPCR is involved in the regulation of myocardial blood flow/hypertension. This protein has a N-terminal Step tag II and an 8X His tag followed by a TEV protease cleavage site.
Information
Target name: Adenosine receptor (A2A receptor)
Catalogue number: PP1
Class: GPCR Class A
Sequence: Full-length, wildtype sequence, with a N-terminus Strep tag II, 8xHis-tag, and TEV protease cleavage site.
Affinity Tag: His/Strep (both N-terminal)
Origin: Human (Homo sapiens)
Theor. MW: 47,7kDa
Accession #: P29274 (UniProt)
Shipment temperature: Dry Ice
Storage conditions: Store at -80°C
Production
Expression system: Sf9 insect cells (baculovirus)
Purity: >90%
Purification: Immobilized Metal Affinity Chromatography
Activity: Confirmed by radiobinding assay
Concentration: Up to 5mg/ml
Sample buffer: 50mM Hepes pH 7.4, 200mM NaCl, 0.05%/0.006% DDM/CHS
Available quantity: From 10µg up to mg scale
Adenosine Receptors : CALIXAR's unique & custom-built approach
CALIXAR’s A2A Adenosine receptors facilitate reliable fragment-based drug design (FBDD), structure-based drug discovery (SBDD) and antibody discovery corresponding to this specific target.
Unlike CALIXAR’s A2A Adenosine receptors, other alternative methods result in an adenosine receptor that becomes mutated and truncated (96 amino-acids truncation in the C-terminus). Additionally, this mutated version becomes locked within an antagonist conformation.
Native Full-Length Adenosine Receptors
CALIXAR’s A2A Adenosine receptor is the first native full-length and functional target on the market. Other existing A2A targets are either mutated or truncated. Our A2A protein is produced in a eukaryotic system with the proper post-translational modifications (glycosylation).
Adenosine Receptors Specifically Made for Biotech
CALIXAR’s A2A Adenosine receptors are high-quality membrane proteins used for (bio)drug discovery and are adapted for use in pharmaceutical, biotechnology companies, and as well as for academic teams that are involved in the life science fields.
Adenosine Receptors For Any Life Science Project
- Antibodies (including nanobodies, scaffold proteins, aptamers)
- Small molecules
- 3D Structures (classical X-ray or XFEL, Cryo-EM, NMR)
- Drug discovery (Screening: HTS, FBDD, SBDD; Hit and lead validation)
- Antibody discovery (Immunization and display technologies)
- Clinical stage (drug validation on reliable native A2A)
As with all GPCRs, the A2A Adenosine receptor is an unstable target and is difficult to produce natively with conventional approaches. Previously, A2A Adenosine receptors could only be locked in one specific conformation (e.g. antagonist) and were only ever prepared in a solution that inherently could not be pure, nor native (truncated, mutated) and without PTMs. A2A’s have only ever been inherently unstable, but not anymore.
Today, CALIXAR’s A2A receptors are able to bind to agonists, antagonists, as well as allosteric modulators (Igonet S. et al., 2018, Scientific Reports). Our A2A receptors also maintain their structural and functional integrity and are purified and stabilized to full length and wild-type (native) proteins.
SCIENTIFIC REPORTS
Enabling STD-NMR fragment screening using stabilized native GPCR : A case study of adenosine receptor
Igonet S et al. 2018
DISCOVERY ON TARGET
Towards Native and Stable GPCRs for Conformational Antibody Development
Jawhari A. Boston, 2015
ANALYTICAL BIOCHEMISTRY
Novel systematic detergent screening method for membrane proteins solubilization.
Desuzinges Mandon E. et al. 2017