Adenosine receptor A2A - Class A GPCR
- Target name: Adenosine receptor A2A (A2AR)
- Gene: ADORA2A
- Uniprot Accession: P29274
- Origin: Human (Homo sapiens)
- Class: Class A GPCR
- Sequence: Full-length, wild type sequence, with a N-terminus Strep tag II, 8xHis-tag, and TEV protease cleavage site.
- Affinity Tag: His/Strep (both N-terminal)
- Catalogue number: PP1
- Theor. MW: 47,7kDa
- Shipment temperature: Dry Ice
- Storage conditions: Store at -80°C
- 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: PBS, 0.05%/0.006% DDM/CHS OR
50mM Hepes pH 7.4, 200mM NaCl, 0.05%/0.006% DDM/CHS - Available quantity: From 10µg up to mg scale
Adenosine receptor A2A: We use a unique & custom-built approach to give us the edge
CALIXAR’s Adenosine receptor A2A facilitates reliable fragment-based drug design (FBDD), structure-based drug discovery (SBDD) and antibody discovery corresponding to this specific target.
Unlike CALIXAR’s Adenosine receptor A2A, 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.
As with all GPCRs, the Adenosine receptor A2A is an unstable target and is difficult to produce natively with conventional approaches. Previously, Adenosine receptor A2A 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. A2AR’s have only ever been inherently unstable, but not anymore.
Today, CALIXAR’s Adenosine receptor A2A is able to bind to agonists, antagonists, as well as allosteric modulators (Igonet S. et al., 2018, Scientific Reports). Our Adenosine receptor A2A also maintain its structural and functional integrity and is purified and stabilized to full length and wild-type (native) proteins.
CALIXAR’s Adenosine receptor A2A is the first native full-length and functional target on the market. Other existing A2AR targets are either mutated or truncated. Our A2AR protein is produced in a eukaryotic system with the proper post-translational modifications (glycosylation).
CALIXAR’s Adenosine receptor A2A high-quality membrane proteins are 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.
- 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)
