G Protein–Coupled Receptors (GPCRs)
G-protein coupled receptors (GPCRs) constitute the largest family of membrane receptors and regulate a broad spectrum of physiological processes, including metabolism, neurotransmission, immune cell trafficking, and endocrine signaling. Due to their central role in cell communication, GPCRs represent one of the most important target classes in drug discovery.
Our GPCR recombinant protein solutions are engineered to support receptor–ligand interaction analysis, pharmacological characterization, and translational research, offering multiple construct strategies tailored to the structural complexity of GPCR biology.
Engineered for GPCR Biology and Drug Discovery
Unlike soluble enzymes or single-pass receptors, GPCRs rely on extracellular ligand recognition, conformational rearrangement, and intracellular signal coupling. This portfolio focuses on providing GPCR formats that enable experimental access to these critical steps.
Ligand Binding and Recognition Studies
Recombinant GPCR extracellular domains (ECDs), particularly for Class B and peptide-binding GPCRs, support direct analysis of ligand binding, specificity, and affinity.
Pharmacology and Target Validation
Defined receptor constructs enable screening and characterization of agonists, antagonists, and biased ligands, supporting early-stage GPCR drug discovery.
Structure–Function and Domain Analysis
Isolated N-terminal or extracellular regions allow focused studies on ligand recognition motifs and receptor activation determinants.
Translational and Disease-Relevant Research
GPCRs such as GCGR, CXCR4, CNR1, and GHR are deeply involved in metabolic regulation, immune cell migration, neurological signaling, and endocrine pathways, making them critical tools for disease mechanism research.
Diverse GPCR Construct Strategies
To address the experimental challenges associated with GPCRs, multiple recombinant formats are provided, each optimized for specific applications.
Available formats include:
- Extracellular domain (N-ECD) constructs for peptide ligand binding and interaction assays
- Fc-fusion proteins to enhance solubility, stability, and avidity
- Biotinylated (Avi-tagged) receptors for immobilization, BLI/SPR, and high-throughput screening
- Detergent-solubilized full-length or extended GPCR constructs for advanced biochemical and structural studies
- Tagged formats (His, Flag, Fc) to support assay compatibility and purification workflows
Construct boundaries are selected based on GPCR class, ligand-binding mode, and known structural features.
Coverage Across GPCR Classes and Species
This portfolio spans multiple GPCR subfamilies and disease-relevant targets, including:
- Class B GPCRs (e.g., Glucagon receptor, GCGR)
- Chemokine receptors (e.g., CXCR4)
- Cannabinoid receptors (e.g., CNR1 / CB1)
- Endocrine and metabolic receptors (e.g., GHR)
Multi-species availability-including human, mouse, and cynomolgus monkey-supports translational studies and preclinical model development.
Mammalian Expression and Controlled Solubilization
Given the folding complexity and post-translational modification requirements of GPCRs, recombinant proteins are produced using mammalian expression systems. For membrane-embedded constructs, optimized detergent and lipid-mimetic conditions are applied to maintain receptor stability and functionality.
This approach supports:
- Native-like folding and extracellular domain integrity
- Compatibility with ligand binding and pharmacological assays
- Reproducible performance across experimental platforms
Quality Attributes Supporting Sensitive GPCR Assays
GPCR assays often involve subtle binding differences and conformational states. Each recombinant protein is manufactured under standardized quality control processes to ensure reliability and reproducibility.
Key quality features include:
- High purity and defined molecular composition
- Low endotoxin levels suitable for cell-based and biochemical assays
- Batch-to-batch consistency
- Clear construct annotation for experimental transparency
Available Recombinant Proteins
Integrated GPCR Research Solutions
This GPCR recombinant protein portfolio is supplied for research use only and is designed to integrate seamlessly into GPCR-focused research and drug discovery workflows. Flexible construct design, disease-relevant target coverage, and application-driven engineering provide reliable support from basic receptor biology to translational studies.
For detailed target availability, construct formats, species options, or technical support, please explore individual product pages or contact our technical support team.
* For research use only. Not intended for any clinical use.