GPCRs are Important Drug Targets
G protein-coupled receptors (GPCRs) are the largest family of human cell-surface receptors. These seven-transmembrane (7TM) proteins are activated by a diverse range of extracellular ligands, including neurotransmitters, odorants, hormones, ions, and photons. Ligand binding causes a conformational change in the GPCR and the subsequent activation of the bound G protein. The activated G proteins stimulate multiple downstream signaling pathways, resulting in the regulation of a variety of physiological processes. GPCR or G protein mutations and abnormal GPCR signaling has been shown to underlie many diseases such as cardiac and inflammatory disorders, metabolic diseases, and cancer. As such, GPCRs have been a common target for therapeutic development. Roughly 35% of drugs approved by the FDA are directed against GPCRs. However, only a small proportion of the 800 GPCRs identified are currently targeted by therapeutics, leaving over 55% of the non-olfactory GPCRs to still be explored as potential drug targets.
GPCR Antibodies for GPCR Drug Development
Expanding the range of therapeutics directed against GPCRs requires highly specific tools for drug discovery, particularly GPCR antibodies. Antibodies are invaluable tools for drug development as they are used for:
- Identification and validation of the biological target
- Assay development
- Patient selection
- Evaluation of cell models
- Verification of consistent analyte expression by engineered cell lines
Since there is great interest in GPCRs as targets for new therapeutics, there is considerable demand for GPCR antibodies. However, antibodies directed against GPCRs are difficult to generate as the receptors are embedded in the plasma membrane, which limits usable immunogenic epitopes and makes the receptors difficult to isolate. As such, many commercially available GPCR antibodies lack the specificity that is needed for the drug development process.
Bio-Techne brand R&D Systems, has been the leader in designing and manufacturing GPCR antibodies for over 20 years. Our antibodies out-perform our competitors because:
- We use whole cell transfectants as immunogens. This allows us to produce antibodies against the full, native GPCR.
- We screen our GPCR antibodies using native GPCR-expressing cells to ensure that our antibodies detect the native protein.
- Our antibody validation protocol is unmatched in the industry. In addition to continually testing lot-to-lot consistency and antibody performance, we confirm antibody specificity using true and irrelevant transfected cells and perform live cell staining to verify detection for low expressing GPCRS.
- About 95% of our 1900+ GPCR antibodies are validated for flow cytometry, allowing you to easily detect receptor expression in your cell models or engineered cell lines.
To learn more about our approach to manufacturing GPCR antibodies visit the R&D Systems Antibodies for G Protein-Coupled Receptors page .
Case Studies Using Bio-Techne GPCR Antibodies
CCR5 Epitope Mapping
CCR5 Epitope Mapping
Authors of a 1999 Journal of Biological Chemistry paper sought to map the epitopes of the chemokine receptor CCR5, a coreceptor for HIV-1, to determine the domains that are involved in binding to the viral envelope glycoprotein. R&D Systems worked with the investigators to generate a panel of CCR5 monoclonal antibodies that can distinguish the different epitopes.
PAR2 Epitope Responsible for Blocking Antibody Binding
PAR2 Epitope Responsible for Blocking Antibody Binding
Authors of a 2017 Nature paper wanted to determine the crystal structure of Protease-Activated Receptor 2 (PAR2) in complex with antagonists to determine allosteric sites that could be used for drug design. R&D Systems worked with the authors to purify the Fab from our Human PAR2 Monoclonal Antibody, which blocks PAR2 activation, so to determine the epitope that is responsible for the antibody’s blocking activity.
Custom Antibody Services
If you can’t find the antibody that you need on our website, contact us. Leverage the experience and skill of our antibody development scientists for your custom antibody project.
Small Molecules And Peptides for Developing GPCR Therapeutics
Tocriscreen GPCR Compound Library
Combining pharmacological and chemical diversity
A curated bioactive compound library of 240 compounds for GPCR research. Designed for high throughput screening, high-content screening, target validation and assay development.
Check out our newly-generated phylogenetic tree.
Small Molecules and Peptides for GPCRs
Small Molecules and Peptides for GPCRs
Bio-Techne brand Tocris, supplies a high-quality small molecules and peptides including potent and selective agonists, and allosteric modulators for investigating the structure, function and signaling of GPCRs. The range contains gold standards and innovative molecules, such as biased agonists, as well as FDA-approved drugs.
Chemokines and Chemokine Receptors
Chemokines and Chemokine Receptors
Chemokines and their G protein-coupled receptors are considered to be highly promising drug targets for the treatment of chronic inflammatory and autoimmune diseases. Explore our wide range of R&D Systems™ bioactive chemokines for investigating chemokine-receptor interactions, signaling pathways, and functions.
GPCR-Related Resources
Interactive GPCR Family Tree
Interactive GPCR Family Tree
Explore this interactive GPCR family tree on the R&D Systems site. The clickable family names link to antibodies and other research tools that we offer for the receptors in that family.